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1. 发明授权

US5182370A Paramagnetic chelates 失效
标题翻译：顺磁螯合物
公开(公告)号：US5182370A
公开(公告)日：1993-01-26
申请号：US450225
申请日：1989-12-13
申请人： Ernst Felder , Luciano Fumagalli , Fulvio Uggeri , Giorgio Vittadini
发明人： Ernst Felder , Luciano Fumagalli , Fulvio Uggeri , Giorgio Vittadini
IPC分类号： A61K49/00 , A61K31/28 , C07C229/22 , C07C229/40 , C07C229/46 , C07C233/10 , C07D401/12 , C07F5/00 , C07F13/00 , C07F15/02
CPC分类号： A61K31/28
摘要： Comounds having the formula ##STR1## wherein: a is 2 or 3; b is an integer from 0 to 4;Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44;E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;S is the group --A--O--R wherein:A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --; m is an integer from 1 to 5; R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hyroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms;R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.2 ; hydroxy-arylalkyl radical in which the aryl radical is unsubstituted or substituted by hydroxy;R.sub.2 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; with the proviso that when R.sub.1 is --CH.sub.2 COOZ or --CH(CH.sub.3)COOZ, R.sub.2 is other than --CH.sub.2 COOZ and --CH(CH.sub.3)--COOZ ##STR2## wherein: R.sub.3 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; a monovalent radical having the structure S--CH--COOZ;X is a direct chemical bond; --O--; --S--; --NH--; --N--CH.sub.2 COOZ; --N--CH(CH.sub.3)COOZ;n is the integer 2 or 3, with the proviso that when X is a direct chemical bond, n is 1, 2 or 3;Z is H or a negative charge;with the proviso that, unless R represents a trifluoromethyl substituted phenyl or R.sub.1 is R.sub.2, Me.sup.(a+) is different from Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+) and Mn.sup.(2+) and with the proviso that when R.sub.1 is R.sub.2 every molecule can contain not more than 500 nitrogen atoms.
摘要翻译：具有式的化合物，其中：a为2或3; b为0〜4的整数; Me（a +）是原子序数为57〜70的元素的离子或原子序数21-29,42或44的过渡金属的离子; E（b +）是无机或有机碱或氨基酸的一种或多种生理生物相容阳离子，所述阳离子表示b单元的总正电荷; S是基团-A-O-R，其中：A是 - （CH 2）m - ; -CH 2 -C（CH 3）2 - ; m为1〜5的整数; R为H; 1至8个碳原子的直链或支链烷基，所述碳原子未被取代或被一个或多个羟基取代; 1至4个脂族碳原子的芳烷基; 苯基或被卤素，氨基，羟基或三氟甲基取代的苯基; 具有1至10个氧原子和3至30个碳原子的（多） - 氧代 - 烷基; R1是R2或-CH2COOZ; -CH（CH 3）COOZ; - （CH 2）n -N（CH 2 COOZ）2; 其中芳基未被取代或被羟基取代的羟基 - 芳基烷基; R2是-CH2COOZ; -CH（CH 3）COOZ; 条件是当R1是-CH2COOZ或-CH（CH3）COOZ时，R2不是-CH2COOZ和-CH（CH3）-COOZ其中：R3是-CH2COOZ; -CH（CH 3）COOZ; 具有结构S-CH-COOZ的单价基团; X是直接化学键; -O-; -S-; -NH-; -N-CH 2 COOZ; -N-CH（CH 3）COOZ; n为整数2或3，条件是当X为直接化学键时，n为1,2或3; Z为H或负电荷; 条件是，除非R代表三氟甲基取代的苯基或R1是R2，Me（a +）不同于Fe（2+），Fe（3+），Gd（3+）和Mn（2+）条件是当R1为R2时，每个分子可含有不超过500个氮原子。

2. 发明授权

US4916246A Paramagnetic chelates useful for NMR imaging 失效
标题翻译：用于NMR成像的顺磁性螯合物
公开(公告)号：US4916246A
公开(公告)日：1990-04-10
申请号：US2115
申请日：1987-01-12
申请人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorgio Vittadini
发明人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorgio Vittadini
IPC分类号： A61K49/00 , A61K31/28 , C07C229/22 , C07C229/40 , C07C229/46 , C07C233/10 , C07D401/12 , C07F5/00 , C07F13/00 , C07F15/02
CPC分类号： A61K31/28
摘要： Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH;R.sub.1 is the same as R.sub.2 oris --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.2, a hydroxy arylalkyl, hydroxy pyridylalkyl, hydroxy aryl(carboxy)alkyl or hydroxy pyridyl-(carboxy)alkyl radical, where the aryl or pyridyl radical may be substituted by hydroxyl, hydroxy alkyl, alkyl, halogen, carboxyl or SO.sub.3 H;R.sub.2 is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, ##STR2## wherein R.sub.3 is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ or a monovalent radical having the structure ##STR3## X is a direct chemical bond, --O--, --S--, --NH--, ##STR4## n is the integer 2 or 3, with the proviso that when X represents a direct bond, n is 1, 2 or 3;Z is hydrogen or a unit of negative charge, and --(CH.sub.2).sub.m -- may also be --CH.sub.2 --C(CH.sub.3).sub.2 --.
摘要翻译：适用于具有下式的NMR成像的化合物：其中a为2或3; b为0〜4的整数; Me（a +）是Fe（2+），Fe（3+），Gd（3+）或Mn（2+）; E（b +）是碱金属，碱土金属，烷基铵，链烷醇铵，多羟基烷基铵或碱性质子化氨基酸的离子，所述离子代表总电荷b; m为1〜5的整数; R是H，具有1至8个碳原子的烷基，具有1至8个碳原子的烷基，其中1至5个碳被OH取代; 具有1至4个脂族碳原子的芳烷基; 苯基或被卤素，羟基，羧基，羧酰胺，酯，SO 3 H，磺酰胺，低级烷基，低级羟基烷基，氨基，酰氨基取代的苯基; 具有1至50个氧原子和3至150个碳原子的（多）氧杂 - 烷基，其中1至5个氢原子可以被OH取代; R1与R2相同或为-CH2COOZ，-CH（CH3）COOZ，CH2CH2-N（CH2COOZ）2，羟基芳基烷基，羟基吡啶基烷基，羟基芳基（羧基）烷基或羟基吡啶基 - （羧基）烷基，芳基或吡啶基可以被羟基，羟基烷基，烷基，卤素，羧基或SO 3 H取代; R2是-CH2COOZ，-CH（CH3）COOZ，其中R3是-CH2COOZ，-CH（CH3）COOZ或具有结构X的单价基团是直接化学键，-O- ，-S-，-NH-， n为整数2或3，条件是当X表示直接键时，n为1,2或3; Z是氢或负电荷的单元， - （CH 2）m - 也可以是-CH 2 -C（CH 3）2 - 。

3. 发明授权

US5132409A Macrocyclic chelating agents and chelates thereof 失效
标题翻译：大环螯合剂及其螯合物
公开(公告)号：US5132409A
公开(公告)日：1992-07-21
申请号：US449883
申请日：1989-11-27
申请人： Ernst Felder , Carlo Musu , Luciano Fumagalli , Fulvio Uggeri
发明人： Ernst Felder , Carlo Musu , Luciano Fumagalli , Fulvio Uggeri
IPC分类号： A61K49/06 , C07D257/02
CPC分类号： A61K49/06 , C07D257/02
摘要： Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. ##STR1##
摘要翻译：其中A为下式（Ⅱ）基团，其中R为H或烷基或任意取代的苄基或H（OCH 2 CH 2）1的式（I）的基团，其通式（I）的1,4,7,10-四氮杂环十二烷的大环衍生物 -4-，Me（OCH 2 CH 2）1-4 - 或Et（OCH 2 CH 2）1-4 - 基，X或O-R 1，其中R 1是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或多氧杂烷基或X是 -NR2R3，其中R2和R3为H或烷基，羟烷基，烷氧基烷基或烷氧基羟烷基，B1，B2和B3与A相同，或为H或下式（III）的基团，其中R4为H或烷基，Y是O-R5基团，其中R5是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或聚氧杂烷基，或Y是-NR6R7基团，其中R6和R7是H或烷基，羟基烷基，烷氧基烷基或烷氧基羟烷基所述衍生物任选地被盐化，并且其络合盐用作药物和/或诊断剂。（一）图像（二）<图像>（三）

4. 发明授权

US4980502A Paramagnetic chelates 失效
标题翻译：顺磁螯合物
公开(公告)号：US4980502A
公开(公告)日：1990-12-25
申请号：US411906
申请日：1989-09-25
申请人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorio Vittadini
发明人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorio Vittadini
IPC分类号： A61K49/00 , A61K31/28 , C07C229/22 , C07C229/40 , C07C229/46 , C07C233/10 , C07D401/12 , C07F5/00 , C07F13/00 , C07F15/02
CPC分类号： A61K31/28
摘要： Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH; R.sub.1 is the same as R.sub.2 or is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.2, a hydroxy arylalkyl, hydroxy pyridylalkyl, hydroxy aryl(carboxy)alkyl or hydroxy pyridyl-(carboxyl)-alkyl radical, where the aryl or pyridyl radical may be substituted by hydroxyl, hydroxy alkyl, alkyl, halogen, carboxyl or SO.sub.3 H; is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, ##STR2## wherein R.sub.3 is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ or a monovalent radical having the structure ##STR3## X is a direct chemical bond, --O--, --S--, 13 NH--, n is the integer 2 or 3, with the proviso that when X represents a direct bond, n is 1, 2 or 3;Z is hydrogen or a unit of negative charge, and --(CH.sub.2).sub.m -- may also be --CH.sub.2 --C(CH.sub.3).sub.2 --.

5. 发明授权

US4588574A Process for the preparation of barium sulfate of increased flowability and density, suitable as a radio-opaque component in radiographic contrast agents, product obtained according to this process and the radiographic contrast agent produced therefrom 失效
标题翻译：用于制备流动性和密度增加的硫酸钡的方法，适合于放射造影剂中的不透射线组分，根据该方法获得的产品和由其制备的放射造影剂
公开(公告)号：US4588574A
公开(公告)日：1986-05-13
申请号：US636399
申请日：1984-07-31
申请人： Ernst Felder , Maria Zingales, deceased
发明人： Ernst Felder , Maria Zingales, deceased
IPC分类号： A61K49/04 , C01F11/46
CPC分类号： A61K49/0404 , C01F11/462 , C01P2006/10 , C01P2006/22
摘要： Barium sulfate suitable for the preparation of radiographic contrast agents of increased flowability and density is obtained by a high temperature treatment at 700.degree. to 1,200.degree. C. and preferably at 800.degree. to 1,000.degree. C. The barium sulfate so sintered is distinguished by a bulk density of 2.5 to 3 g/ml and its aqueous suspension, containing 200 g of barium sulfate per 100 ml, is distinguished by a viscosity of no more than 1,000 mPas. Radiographic contrast agents containing at least 200 g of sintered barium sulfate per 100 ml are outstandingly suitable for the difficult double contrast visualization of the stomach and gastric mucosa.
摘要翻译：适用于制备增加流动性和密度的放射造影剂的硫酸钡是通过700至1200℃，优选800至1000℃的高温处理获得的。如此烧结的硫酸钡的体积大小密度为2.5至3g / ml及其含水悬浮液，每100ml含有200g硫酸钡，其粘度不超过1,000mPas。含有至少200克烧结硫酸钡/ 100毫升的放射造影剂显着适用于胃和胃粘膜的困难的双重对比度可视化。

6. 发明授权

US4246164A Process for the resolution of (+)- and (-)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid 失效
标题翻译：（+） - 和（ - ） - 6-甲氧基-α-甲基-2-萘乙酸的分离方法
公开(公告)号：US4246164A
公开(公告)日：1981-01-20
申请号：US55427
申请日：1979-07-06
申请人： Ernst Felder , Davide Pitre , Hans Zutter
发明人： Ernst Felder , Davide Pitre , Hans Zutter
IPC分类号： C07C59/64 , C07B31/00 , C07B57/00 , C07C51/00 , C07C51/487 , C07C51/64 , C07C53/136 , C07C67/00 , C07C91/10 , C07B19/00 , C07C65/24
CPC分类号： C07C51/487 , Y02P20/582
摘要： The subject of the invention is a process for resolving mixtures of (+)- and (-)-6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid into the enantiomers thereof, characterized in that N-methyl-D-glucamine [=1-deoxy-1-(methylamino)-D-glucitol] is used as the resolving agent, so that the 6-methoxy-.alpha.-methyl-2-naphthaleneacetic acid is converted into the corresponding diastereoisomeric N-methyl-D-glucamine salt pair which, because of very different solubilities, can be separated easily and completely with high yield.
摘要翻译：本发明的主题是将（+） - 和（ - ） - 6-甲氧基-α-甲基-2-萘乙酸的混合物分解成其对映异构体的方法，其特征在于N-甲基-D-葡糖胺[= 使用1-脱氧-1-（甲基氨基）-D-葡萄糖醇作为拆分剂，使得6-甲氧基-α-甲基-2-萘乙酸转化为相应的非对映异构体N-甲基-D-葡糖胺盐由于非常不同的溶解度，可以容易且完全地以高收率分离。

7. 发明授权

US5710271A Process for the preparation and separation of diastereomeric salts of folinic acid 失效
标题翻译：制备和分离亚叶酸非对映体盐的方法
公开(公告)号：US5710271A
公开(公告)日：1998-01-20
申请号：US480097
申请日：1995-06-07
申请人： Ernst Felder , Giorgio Ripa , Carlo Distaso
发明人： Ernst Felder , Giorgio Ripa , Carlo Distaso
IPC分类号： C07D475/04
CPC分类号： C07D475/04
摘要： A process for the preparation, separation and purification of (6S) and (6R) diastereomers of folinic acid salts with at least dibasic amines is disclosed, which process comprises the hydrolysis of (6RS)-5,10-methenyl-5,6,7,8-tetrahydrofolic acid chloride hydrochloride with an at least dibasic amine and the subsequent separation of the diasteromeric salts.
摘要翻译：公开了用至少二元胺制备，分离和纯化亚叶酸盐的（6S）和（6R）非对映异构体的方法，该方法包括（6RS）-5,10-间苯基-5,6， 7,8-四氢叶酸酰氯盐酸盐与至少二元胺反应，随后分离非对映体盐。

8. 发明授权

US5023379A Process for the preparation of hydroxyamines 失效
标题翻译：羟基胺的制备方法
公开(公告)号：US5023379A
公开(公告)日：1991-06-11
申请号：US492018
申请日：1990-03-12
申请人： Ernst Felder , Michael Romer , Hans Bardonner , Hartmut Hartner , Wolfgang Fruhstorfer
发明人： Ernst Felder , Michael Romer , Hans Bardonner , Hartmut Hartner , Wolfgang Fruhstorfer
IPC分类号： C07B61/00 , B01J23/00 , B01J23/40 , B01J23/44 , B01J25/00 , B01J25/02 , C07C20060101 , C07C67/00 , C07C209/26 , C07C213/00 , C07C213/02 , C07C215/06 , C07C215/10 , C07C215/12 , C07C249/02
CPC分类号： C07C215/10 , C07C213/02 , C07C249/02
摘要： A process for the production of hydroxyamines of the formula IR.sup.1 --CH(OH)--CH(NHR.sup.3)--R.sup.2 (I)whereinR.sup.1 and R.sup.2 independently of one another are H or CH.sub.2 OH andR.sup.3 is H, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -hydroxyalkyl comprising reacting an oxo compound with an amine and reducing the resultant ketimine with a reducing agent.
摘要翻译：制备式I的基团的方法R1-CH（OH）-CH（NHR3）-R2（Ⅰ）其中R1和R2彼此独立地是H或CH2OH，R3是H，C1-C4烷基或包括将氧代化合物与胺反应并用还原剂还原所得的酮亚胺的C 1 -C 4 - 羟烷基。

9. 发明授权

US4139605A Water-soluble, non-ionizing, radiopaque compounds and contrast compositions containing the same 失效
标题翻译：水溶性，非电离，不透射线的化合物和含有它们的对比组合物
公开(公告)号：US4139605A
公开(公告)日：1979-02-13
申请号：US881567
申请日：1978-02-27
申请人： Ernst Felder , Davide Pitre
发明人： Ernst Felder , Davide Pitre
IPC分类号： A61K49/04 , C07C67/00 , C07C231/00 , C07C231/02 , C07C233/12 , C07C237/46 , A61K29/02 , C07C103/24 , C07C103/26 , C07C103/28
CPC分类号： C07C233/12
摘要： .alpha., .omega.-BIS-[5-(DIHYDROXYALKYL) AMINOCARBONYL-3-HYDROXYACYL-AMINO-2,4,6-TRIIODO-BENZOYL-AMINO]-OXAALKANE COMPOUNDS OF THE FORMULA ##STR1## wherein R.sub.1 is ##STR2## R and R' are hydrogen or methyl, R.sub.2 is dihydroxyalkyl having 3 or 4 carbon atoms,N is 2 or 3,M is an integer between 1 and 5, andN(m+1) is an integer between 4 and 12,Are readily soluble in water to yield injectable radiopaque contrast compositions which are well tolerated and stable. The compounds are prepared in good yields by reacting a reactive derivative of a 5-(di-hydroxyalkyl)aminocarbonyl-3-acyloxyacylamino-2,4,6-triiodo-benzoic acid with an .alpha.,.omega.-diamino-oxaalkane of the formulaR--NH--C.sub.n H.sub.2n --(O--C.sub.n H.sub.2n)--NH--R.
摘要翻译： α，ω-BIS- [5-（二羟基烷基）氨基]苯甲酰基-3-羟基酰胺 - 氨基-2,4,6-三羟基苯甲酰氨基] - 奥卡康化合物，其中R1是R和R “是氢或甲基，R2是具有3或4个碳原子的二羟基烷基，N IS 2 OR 3，M是1和5之间的整数，N（M + 1）是4和12之间的整数，可以是易溶于防水耐受性强的对比组合物，易于耐受和稳定。通过使5-（二羟烷基）氨基羰基-3-酰氧基酰基氨基-2,4,6-三碘 - 苯甲酸的反应性衍生物与式R的α，ω-二氨基 - 氧杂烷反应，以良好的收率制备化合物 -NH-C n H 2n - （O-C n H 2n）-NH-R。

10. 发明授权

US4503252A Process for the preparation of serinol and of serinol derivatives, and products obtained therefrom 失效
标题翻译：丝氨醇和丝氨醇衍生物的制备方法以及由此得到的产物
公开(公告)号：US4503252A
公开(公告)日：1985-03-05
申请号：US441777
申请日：1982-11-15
申请人： Ernst Felder , Sergio Bianchi , Heinrich Bollinger
发明人： Ernst Felder , Sergio Bianchi , Heinrich Bollinger
IPC分类号： C07C213/00 , C07C67/00 , C07C213/02 , C07C215/10 , C07D295/088 , C07C85/04 , C07C85/24
CPC分类号： C07D295/088
摘要： A method for the synthesis of serinol and serinol derivatives substituted at the nitrogen atoms by reacting a lower 1,3-dialkoxy-isopropyl halide with ammonia or an amine to form a 1,3-dialkoxy-isopropylamine and then removing the ether groups by heating with a hydrogen halide acid. The method allows the production of serinol and serinol derivatives using inexpensive starting materials in a simple manner and obtaining a high purity product which is free of interfering isomers. Novel compounds obtained by the method which are useful as pharmaceutical intermediates, X-ray contrasting agents and cytostatic or psychopharmacological drugs are also disclosed.
摘要翻译：通过使低级1,3-二烷氧基 - 异丙基卤化物与氨或胺反应形成1,3-二烷氧基 - 异丙胺，然后通过加热除去醚基，合成在氮原子上取代的丝氨醇和丝氨醇衍生物的方法与卤化氢酸反应。该方法允许以简单的方式使用廉价的原料生产丝氨醇和丝氨醇衍生物，并获得不含干扰异构体的高纯度产物。还公开了通过可用作药物中间体，X射线造影剂和细胞抑制剂或精神药物药物的方法获得的新型化合物。

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