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1. 发明授权

US5625064A Process for the preparation of triazolones 失效
标题翻译：制备三唑酮的方法
公开(公告)号：US5625064A
公开(公告)日：1997-04-29
申请号：US458550
申请日：1995-06-02
申请人： David R. Andrews , Dinesh Gala , Jacques Gosteli , Frank Guenter , William Leong , Ingrid Mergelsberg , Anantha Sudhakar
发明人： David R. Andrews , Dinesh Gala , Jacques Gosteli , Frank Guenter , William Leong , Ingrid Mergelsberg , Anantha Sudhakar
IPC分类号： C07D249/12 , C07D521/00 , C07D403/10
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/12
摘要： Described is a process for preparing triazolone compounds of the formula ##STR1## comprising heating a mixture of a compound of the formula ##STR2## and a hydrazine derivative of the formula R.sup.5 --NH--NH--CHO, R.sup.5 --NH--NH--C(O)OC(CH.sub.3).sub.3 or R.sup.5 --NH--NH--C(O)OCH.sub.2 C.sub.6 H.sub.5, optionally in the presence of an added base.
摘要翻译：描述了制备下式的三唑酮化合物的方法：包括加热式IMA化合物与式R 5 -NH-NH-CHO，R 5 -NH-NH-C（ O）OC（CH 3）3或R 5 -NH-NH-C（O）OCH 2 C 6 H 5，任选地在加入的碱的存在下。

2. 发明授权

US5455363A Amino acid derivatives for peptide synthesis 失效
标题翻译：用于肽合成的氨基酸衍生物
公开(公告)号：US5455363A
公开(公告)日：1995-10-03
申请号：US957677
申请日：1992-10-07
申请人： Jacques Gosteli , Beat Sax , Fritz Dick , Rudolf Tanner
发明人： Jacques Gosteli , Beat Sax , Fritz Dick , Rudolf Tanner
IPC分类号： C07C237/06 , C07C271/22 , C07K1/06 , C07K7/04
CPC分类号： C07C237/06 , C07C271/22 , C07K1/066 , C07C2103/18 , Y02P20/55
摘要： Compounds of formula I are described, ##STR1## wherein n is equal to one or two, R.sub.1 stands for hydrogen or an amino protecting group, R.sub.2 represents hydrogen or a carboxyl protecting group and R.sub.3 4-methyltriphenylmethyl, 4,4'-dimethyltriphenylmethyl, 4,4',4"-trimethyltriphenylmethyl. Furthermore described are compounds of formula I which are reactive and suitable for coupling reactions and are derived from I with R.sub.2 =H by activation of the carboxyl group.The compounds mentioned above can be used as starting materials for the synthesis of peptides. They are more suitable than analogous compounds of formula I, wherein R.sub.3 represents hydrogen or a carbamoyl protecting group used hitherto.
摘要翻译：描述式I化合物，其中n等于1或2，R1代表氢或氨基保护基，R2代表氢或羧基保护基，R3,4-甲基三苯基甲基，4,4'-二甲基三苯基甲基，4,4'，4“ - 三甲基三苯基甲基。此外还描述了反应性和适用于偶联反应的式I化合物，并且通过活化羧基得到R 2 = H的I化合物。上述化合物可以用作合成肽的起始原料。它们比类似式I化合物更合适，其中R 3表示氢或迄今使用的氨基甲酰基保护基。

3. 发明授权

US4500457A Process for preparing thia-aza compounds with a beta-lactam ring 失效
标题翻译：用β-内酰胺环制备噻唑化合物的方法
公开(公告)号：US4500457A
公开(公告)日：1985-02-19
申请号：US353288
申请日：1982-03-01
申请人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
发明人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
IPC分类号： C07D205/09 , C07D499/88 , C07F9/568 , C07D501/02
CPC分类号： C07F9/5683 , C07D205/09 , C07D499/88
摘要： 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group,1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.
摘要翻译：其中R 1表示氢，通过碳原子键合到环碳原子上的有机基团或醚化的巯基，R 2表示羟基或基团R 2 A的2-蒎烯-3-羧酸化合物与羰基-C（= O） - 被保护的羧基，其1-氧化物以及具有成盐基团的化合物的盐以外消旋和旋光形式一起形成，其制备方法，药物组合物含有这些化合物及其作为抗生素的用途，以及可用于制备式I化合物的中间体及其方法。

4. 发明授权

US4396621A Certain 2-oxo-2,3-dihydro-3-benzothiophene-carboxamides and their pharmaceutical compositions 失效
标题翻译：某些2-氧代-2,3-二氢-3-苯并噻吩 - 甲酰胺及其药物组合物
公开(公告)号：US4396621A
公开(公告)日：1983-08-02
申请号：US204747
申请日：1980-11-07
申请人： Raymond Bernasconi , Pier G. Ferrini , Richard Goschke , Jacques Gosteli
发明人： Raymond Bernasconi , Pier G. Ferrini , Richard Goschke , Jacques Gosteli
IPC分类号： C07D333/36 , C07D333/64 , C07D333/68 , C07D333/70 , A61K31/425 , C07D409/12
CPC分类号： C07D333/36 , C07D333/64 , C07D333/68 , C07D333/70
摘要： Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]-thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.
摘要翻译：式（Ⅰ）的氧化噻吩化合物，特别是2-氧代-2,3-二氢 - 苯并[b] - 噻吩化合物，其中Ph代表任意取代的1,2-亚苯基，X代表氧或硫， R1表示通过碳原子键合的有机基团，R 2表示氢或任选取代的具有脂族特征的烃基，其盐可用作外周止痛剂和/或作为消炎性尿酸和/或溶栓剂。

5. 发明授权

US4249027A Process for the preparation of 5-substituted resorcinols and related intermediates 失效
标题翻译： 5-取代的间苯二酚和相关中间体的制备方法
公开(公告)号：US4249027A
公开(公告)日：1981-02-03
申请号：US737377
申请日：1976-11-01
申请人： Jacques Gosteli
发明人： Jacques Gosteli
IPC分类号： C07C69/88 , C07C37/50 , C07C39/08 , C07C51/09 , C07C39/12
CPC分类号： C07C51/09 , C07C37/50
摘要： According to the present invention, 5-substituted resorcinols of the formula I ##STR1## wherein R.sub.1 represents a hydrocarbon radical, optionally unsubstituted or substituted by inert substituents, are prepared by reacting a carboxylic acid ester of the formula IIR.sub.1 --C.tbd.C--CO--O--R.sub.2 (II)wherein R.sub.2 represents a non-aromatically bound lower hydrocarbon radical, in the presence of an alkaline condensation agent, with a diester of 3-oxoglutaric acid of the formula IIIR.sub.3 --O--CO--CH.sub.2 --CO--CH.sub.2 --CO--O--R.sub.4 (III)wherein R.sub.3 and R.sub.4 represent non-aromatically bound lower hydrocarbon radicals; hydrolyzing the resulting dihydroxyisophthalic acid acid ester of the formula IV ##STR2## and decarboxylating the hydrolyzed product, a specific embodiment is the preparation of 5-pentylresorcinol.
摘要翻译：根据本发明，式I的5-取代的间苯二酚（I）其中R 1表示任选未被取代或被惰性取代基取代的烃基，通过使式II的羧酸酯R1-C 其中R 2表示非芳香结合的低级烃基，在碱性缩合剂的存在下，与式III的3-氧代戊二酸的二酯R 3 -O-CO- CH2-CO-CH2-CO-O-R4（Ⅲ）其中R3和R4代表非芳香结合的低级烃基; 水解所得的式IV（IV）的二羟基间苯二酸酸酯并使水解产物脱羧，具体实施方案是5-戊基间苯二酚的制备。

6. 发明授权

US4151170A Process for the manufacture of indigoid dyes 失效
标题翻译：靛蓝染料的制造方法
公开(公告)号：US4151170A
公开(公告)日：1979-04-24
申请号：US751223
申请日：1976-12-16
申请人： Jacques Gosteli
发明人： Jacques Gosteli
IPC分类号： C09B7/00 , C07C67/00 , C07C201/00 , C07C205/45 , C09B7/02 , D06P1/28 , D06P3/60
CPC分类号： C09B7/02
摘要： A process for the manufacture of indigoid dyes, wherein a functional derivative of the anthranilic acid of the general formula I ##STR1## in which A completes a mono- or polynuclear, substituted or unsubstituted aromatic ring,X represents a hydrogen atom or a protective group for the free amino group which can form an anhydro derivative with the carboxyl group in the ortho-position,Is reacted with nitromethane in the presence of a base or with a salt of nitroacetic acid to give the .omega.-nitro-o-amino-acetophenone derivative of the general formula II ##STR2## in which A and X are as defined in formula I, and this intermediate is condensed by heating with acids to give the indigo compound of the general formula III ##STR3## in which A is as defined in formula I.
摘要翻译：靛蓝染料的制备方法，其中通式Ⅰ的邻氨基苯甲酸的功能性衍生物（I）其中A完成单或多核，取代或未取代的芳环，X表示氢原子或可以在邻位形成具有羧基的脱水衍生物的游离氨基的保护基，在碱存在或与硝酸盐存在下与硝基甲苯反应以产生ω-NITRO-O- 其中A和X如式I所定义的通式II（II）的氨基 - 乙炔酮衍生物，并且该中间体通过与酸加热而缩合，得到通式III的靛蓝化合物（IMAGE）（ III）其中A如式I所定义。

7. 发明授权

US4070477A 2-Penem compounds 失效
标题翻译： 2-Penem化合物
公开(公告)号：US4070477A
公开(公告)日：1978-01-24
申请号：US746979
申请日：1976-12-02
申请人： Ivan Ernest , Jacques Gosteli , Robert Burns Woodward
发明人： Ivan Ernest , Jacques Gosteli , Robert Burns Woodward
IPC分类号： C07D499/04 , A61K31/397 , A61K31/43 , A61P31/04 , C07D205/08 , C07D205/095 , C07D403/04 , C07D499/21 , C07D499/44 , C07D499/88 , C07F9/568 , A61K31/425 , C07D499/02
CPC分类号： C07D499/88 , C07D205/095 , C07F9/5683 , Y02P20/55
摘要： The invention relates to 6-amino-2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1.sup.a denotes hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl radical Ac, or in which R.sub.1.sup.a and R.sub.1.sup.b conjointly form a bivalent amino protective group, R.sub.2 denotes hydroxyl or a radical R.sub.2.sup.A which, together with the carbonyl grouping --C(.dbd.0)--, forms a protected carboxyl group, and R.sub.3 represents hydrogen or an organic radical which is linked via a carbon atom to the ring carbon atom, and 1-oxides thereof, as well as salts of such compounds having salt-forming groups, which compounds possess antibiotic properties, processes for the manufacture of such compounds, and also pharmaceutical formulations containing compounds of the formula I with pharmacological properties, and the use thereof, either as antibiotics, preferably in the form of pharmaceutical formulations, or as intermediate products.
摘要翻译：本发明涉及式（I）的6-氨基-2-青霉烯-3-羧酸化合物，其中R 1a表示氢或氨基保护基R 1A和R 1b表示氢或酰基Ac，或其中 R1a和R1b共同形成二价氨基保护基，R2表示羟基或R2A基团，与羰基-C（= O）一起形成保护的羧基，R3表示氢或连接的有机基团通过碳原子与环碳原子及其1-氧化物，以及具有成盐基团的化合物的盐，该化合物具有抗生素性质，制备这些化合物的方法，以及含有化合物的化合物的药物制剂具有药理学性质的式I及其用途，优选为药物制剂形式的抗生素或作为中间产物。

8. 发明授权

US5536841A Process for the preparation of 2-substituted 5-chloroimidazole-4-carbaldehydes 失效
标题翻译： 2-取代的5-氯咪唑-4-甲醛的制备方法
公开(公告)号：US5536841A
公开(公告)日：1996-07-16
申请号：US492444
申请日：1995-06-19
申请人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
发明人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
IPC分类号： C07D233/68 , C07D233/70 , C07D233/96 , C07D233/32
CPC分类号： C07D233/96 , C07D233/68
摘要： A process for preparing 2-substituted 5-chloroimidazole-4-carbaldehydes of the general formula: ##STR1## In the process, a glycine ester hydrohalide is ring-closed with an imidate ester to obtain the intermediate 2-substituted 3,5-dihydroimidazol-4-one. This intermediate is converted with an N,N-substituted formamide acetel into an N,N-substituted aminomethyleneimidazolinone. This latter intermediate is chlorinated with phosphorus oxychloride or phosgene to obtain the final product 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula I.Also disclosed are N,N-substituted aminomethyleneimidazolinones of the general formula: ##STR2## wherein R is hydrogen or is an alkyl group, an alkenyl group, a cycloalkyl group, an arylalkyl group or an aryl group, and R.sub.5 and R.sub.6 are identical or different and each is an alkyl group or an aryl group, in the form of the E- or Z-isomer.
摘要翻译：制备以下通式的2-取代的5-氯咪唑-4-甲醛的方法：在该方法中，甘氨酸酯氢卤化物与亚氨酸酯酯闭环，得到中间体2-取代的3,5-二二氢咪唑-4-酮。该中间体用N，N-取代的甲酰胺乙缩醛转化成N，N-取代的氨基亚甲基咪唑啉酮。将后一中间体用磷酰氯或光气氯化，得到通式I的最终产物2-取代的5-氯咪唑-4-甲醛。还公开了通式如下的N，N-取代的氨基亚甲基咪唑啉酮其中 R是氢或是烷基，烯基，环烷基，芳基烷基或芳基，R 5和R 6相同或不同，各自为烷基或芳基，其形式为E - 或Z-异构体。

9. 发明授权

US5486617A Process for the preparation of 2-substituted 5-chloroimidazole-4-carbaldehydes 失效
标题翻译： 2-取代的5-氯咪唑-4-甲醛的制备方法
公开(公告)号：US5486617A
公开(公告)日：1996-01-23
申请号：US340377
申请日：1994-11-14
申请人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
发明人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
IPC分类号： C07D233/68 , C07D233/70 , C07D233/96
CPC分类号： C07D233/96 , C07D233/68
摘要： A process for preparing 2-substituted 5-chloroimidazole-4-carbaldehydes of the general formula: ##STR1## In the process, a glycine ester hydrohalide is ring-closed with an imidate ester to obtain the intermediate 2-substituted 3,5-dihydroimidazol-4-one. This intermediate is converted with an N,N-substituted formamide acetal into an N,N-substituted aminomethyleneimidazolinone. This latter intermediate is chlorinated with phosphorus oxychloride or phosgene to obtain the final product 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula I.Also disclosed are N,N-substituted aminomethyleneimidazolinones of the general formula: ##STR2## wherein R is hydrogen or is an alkyl group, an alkenyl group, a cycloalkyl group, an arylalkyl group or an aryl group, and R.sub.5 and R.sub.6 are identical or different and each is an alkyl group or an aryl group, in the form of the E- or Z-isomer.
摘要翻译：制备以下通式的2-取代的5-氯咪唑-4-甲醛的方法：在该方法中，甘氨酸酯氢卤化物与亚氨酸酯酯闭环，得到中间体2-取代的3,5-二二氢咪唑-4-酮。该中间体用N，N-取代的甲酰胺缩醛转化成N，N-取代的氨基亚甲基咪唑啉酮。将后一中间体用磷酰氯或光气氯化，得到通式I的最终产物2-取代的5-氯咪唑-4-甲醛。还公开了通式如下的N，N-取代的氨基亚甲基咪唑啉酮其中 R是氢或是烷基，烯基，环烷基，芳基烷基或芳基，R 5和R 6相同或不同，各自是烷基或芳基，其形式为E - 或Z-异构体。

10. 发明授权

US4952690A 6-substituted thia-aza compounds 失效
标题翻译： 6-取代的硫杂杂环化合物
公开(公告)号：US4952690A
公开(公告)日：1990-08-28
申请号：US396783
申请日：1989-08-21
申请人： Jacques Gosteli , Ivan Ernest , Marc Lang , Robert B. Woodward
发明人： Jacques Gosteli , Ivan Ernest , Marc Lang , Robert B. Woodward
IPC分类号： A61K31/397 , A61K31/43 , A61P31/04 , C07D205/08 , C07D205/09 , C07D417/12 , C07D499/04 , C07D499/06 , C07D499/86 , C07D499/861 , C07D499/87 , C07D499/88 , C07D499/881 , C07D499/883 , C07D499/887 , C07D499/897 , C07F9/568
CPC分类号： C07D499/88 , C07D205/08 , C07D205/09 , C07F9/5683
摘要： The invention relates to azetidin-2-ones of the formula ##STR1## wherein R.sub.a represents hydroxy-lower alkyl, R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group, R.sub.2.sup.A together with the carbonyl group to which it is attached is a protected carboxyl group and Z' is oxygen, sulfhur or an optionally substituted methylidene group, functional groups in the radicals R.sub.a, R.sub.1 and Z' optionally being in protected form. The azetidinones are useful intermediates for the preparation of penem antibiotics.

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