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1. 发明授权

US4933290A Process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
标题翻译：外消旋恶唑烷酮衍生物的光学异构体的酶分离方法
公开(公告)号：US4933290A
公开(公告)日：1990-06-12
申请号：US137721
申请日：1987-12-24
申请人： Pietro Cesti , Daniele Bianchi , Franco Francalanci , Walter Cabri
发明人： Pietro Cesti , Daniele Bianchi , Franco Francalanci , Walter Cabri
IPC分类号： C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C12P41/004
摘要： There is disclosed a process for the biotechnological resolution, by enzymatic esterification of the corresponding racemic mixture of the S(+) and R(-) optical isomers of the oxazolidinonic compounds having formula (I): ##STR1## wherein R represents a, linear or branched, C.sub.1 -C.sub.8 alkyl group, which process is characterized in that, the racemic 3-alkyl-5-hydroxymethyl-oxazolidin-2-one derivative of formula (I) is reacted with an esterifying compound, selected from esters having formula (III): ##STR2## wherein R represents a, linear or branched, C.sub.1 -C.sub.10 alkyl or alkenyl group and R" represents a linear or branched, C.sub.1 -C.sub.4 alkyl, alkenyl group, a haloalkyl (chlorine, bromine) group or a diacyl glycerolic group or from acids having formula (IV):R'"--COOH (IV)wherein R'" represents a, linear or branched, C.sub.1 -C.sub.20 alkyl or alkenyl group or from anhydrides having formula (V): ##STR3## wherein R.sup.IV represents a, linear or branched, C.sub.1 -C.sub.6 alkyl group, in the presence of an enzyme, immobilized on a porous carrier, capable of giving rise selectively to the esterification reaction of the R(-) isomer, while leaving the S(+) isomer substantially unchanged, which latter is then separated according to known techniques.

2. 发明授权

US4980291A Process for the enzymatic separation of the optical isomers of racemic .alpha.-alkyl-substituted primary alcohols 失效
标题翻译：用于酶分离外消旋的α-烷基取代的伯醇的光学异构体的方法
公开(公告)号：US4980291A
公开(公告)日：1990-12-25
申请号：US307913
申请日：1989-02-09
申请人： Daniele Bianchi , Pietro Cesti , Franco Francalanci , Walter Cabri
发明人： Daniele Bianchi , Pietro Cesti , Franco Francalanci , Walter Cabri
IPC分类号： C12P7/62 , C12P41/00
CPC分类号： C12P41/004 , C12P7/62
摘要： Biotechnological resolution by means of enzymatic transesterification of the relevant racemic mixture of the optical isomers of .alpha.-alkyl-substituted primary alcohols having the formula (I): ##STR1## wherein: R represents a linear or branched (C.sub.1 -C.sub.20)-alkyl or alkenyl group or an aryl group, also substituted or condensed with other groups, in particular a group of formula (II) or (III): ##STR2## wherein: R.sup.ii represents a (C.sub.1 -C.sub.8)-alkyl group, a (C.sub.1 -C.sub.4)-alkenyl group, an alkoxy, phenyl, phenoxy, benzoyl, or heterocyclic group;R.sup.iii represents a hydrogen or halogen atom;R.sup.iv represents a (C.sub.1 -C.sub.4)-alkyl group, and whereinR.sup.i represents a (C.sub.1 -C.sub.4)-alkyl group either equal to, or different from, R,in the presence of an enzyme either free or immobilized on a support capable of selectively causing the S isomer to be esterified, with the R isomer being left substantially unchanged, said isomers being then separated according to techniques known from the prior art. The process is used in the synthesis of antiinflammatory agents.

3. 发明授权

US5215891A Process for preparing penems 失效
标题翻译：制作青铜器的过程
公开(公告)号：US5215891A
公开(公告)日：1993-06-01
申请号：US845800
申请日：1992-03-09
申请人： Maria Altamura , Pietro Cesti , Franco Francalanci , Marcello Marchi , Marco Foa' , Stefano Cambiaghi , Franco Dallatomasina
发明人： Maria Altamura , Pietro Cesti , Franco Francalanci , Marcello Marchi , Marco Foa' , Stefano Cambiaghi , Franco Dallatomasina
IPC分类号： C07D499/88 , C12P37/00
CPC分类号： C07D499/88 , C12P37/00 , Y02P20/55
摘要： A process for preparing a compound of formula I: ##STR1## wherein R.sub.1 represents a hydroxy protecting group and R.sub.2 represents a carboxy protecting group, which comprises:hydrolyzing a compound of formula II ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R represents an alkyl, alkenyl or phenylalkyl group having from 1 to 18 carbon atoms, in the presence of an enzyme capable of selectively hydrolyzing the ester group of the 2-substituent thereof.
摘要翻译：制备式I化合物的方法：其中R 1表示羟基保护基，R 2表示羧基保护基，其包括：水解式II化合物（II），其中R 1和R 2 在具有能够选择性水解其2-取代基的酯基的酶的存在下，R代表具有1至18个碳原子的烷基，烯基或苯基烷基。

4. 发明授权

US5248601A Process for preparing L(-)-carnitine chloride 失效
标题翻译：制备L（ - ） - 肉碱氯化物的方法
公开(公告)号：US5248601A
公开(公告)日：1993-09-28
申请号：US595670
申请日：1990-10-09
申请人： Franco Francalanci , Marco Ricci , Pietro Cesti , Carlo Venturello
发明人： Franco Francalanci , Marco Ricci , Pietro Cesti , Carlo Venturello
IPC分类号： C12P17/02 , C12P41/00
CPC分类号： C12P17/02 , C12P41/005
摘要： A biotechnological process for preparing L(-)-carnitine chloride, having the formula ##STR1## comprising: (a) reacting a racemic ester of (R,S)-3,4-epoxybutyric acid having the formula ##STR2## wherein R is an alkyl group having from 1 to 10 carbons or a benzyl group, with an enzyme capable of selectively hydrolyzing enantiomer S(-);(b) separating the enantiomer S(-) from non-reacted ester which is present in predominantly the R(+) form;(c) reacting the non-reacted ester obtained in step (b) with an enzyme capable of quantitatively hydrolyzing the R(+) form to obtain thereby a salt of 3,4-epoxybutyric acid in the R(+) form having the formula ##STR3## wherein X is Na, K, or Li; (d) reacting the salt obtained in step (c) with a molar excess of trimethylamine; and(e) treating the reaction product of step (d) with HCl to remove excess trimethylamine and to obtain thereby the L(-)-carnitine chloride of formula (I).
摘要翻译：用于制备具有式（I）的L（ - ） - 肉碱氯化物的生物技术方法包括：（a）使具有式（IMA）的（R，S）-3,4-环氧丁酸的外消旋酯与式（II）其中R为具有1至10个碳原子的烷基或苄基，具有能够选择性水解对映体S（ - ）的酶; （b）从主要为R（+）形式存在的未反应的酯分离对映体S（ - ）; （c）将步骤（b）中获得的未反应的酯与能够定量水解R（+）形式的酶反应，从而得到具有式（B）的R（+）形式的3,4-（环己基）（III）其中X是Na，K或Li; （d）使步骤（c）中获得的盐与摩尔过量的三甲胺反应; 和（e）用HCl处理步骤（d）的反应产物以除去过量的三甲胺，从而得到式（I）的L（ - ） - 肉碱氯化物。

5. 发明授权

US4865771A Process for preparing L(-)-carnitine chloride from 3,4-epoxybutyric esters and novel intermediate compounds 失效
标题翻译：从3,4-环氧丁酸酯和新型中间体化合物制备L（ - ） - 肉碱氯化物的方法
公开(公告)号：US4865771A
公开(公告)日：1989-09-12
申请号：US25351
申请日：1987-03-13
申请人： Franco Francalanci , Marco Ricci , Pietro Cesti , Carlo Venturello
发明人： Franco Francalanci , Marco Ricci , Pietro Cesti , Carlo Venturello
IPC分类号： C07D303/40 , C07C20060101 , C07C67/00 , C07C227/00 , C07C227/08 , C07C227/18 , C07C229/22 , C12P13/00 , C12P17/02 , C12P41/00 , C12R1/06 , C12R1/07 , C12R1/38 , C12R1/645 , C12R1/72
CPC分类号： C12P41/005 , C12P17/02
摘要： A process for preparing L(-)-carnitine chloride having the formula: ##STR1## comprising the steps of: (a) reacting a racemic ester of (R,S)-3,4-epoxybutyric acid having the formula: ##STR2## wherein R is an alkyl group having from 1-10 carbons, or a benzyl group, with an enzyme capable of selectively hydrolyzing enantiomer S(-),(b) separating said enantiomer S(-), from non-reacted ester, which is predominantly in the R(+) form;(c) reacting (1) the non-reacted ester obtained in step (b) with trimethylamine hydrochlorid or (2) the trimethylamine, to obtain thereby an ester having the formula: ##STR3## (d) hydrolyzing the ester obtain in step (c) in the presence of HCl to obtain thereby the L(-)-carnitine chloride having formula (I).The present invention is also directed to a novel class of compounds comprising R(+) enantiomers of the esters of 3,4-epoxybutyric acid.
摘要翻译：一种具有下式的制备L（ - ） - 肉碱氯化物的方法：（I）包括以下步骤：（a）使具有下式的（R，S）-3,4-环氧丁酸的外消旋酯：（II）其中R是具有1-10个碳原子的烷基或苄基，具有能够选择性水解对映异构体S（ - ）的酶，（b）将所述对映异构体S（ - ）与非 - 主要是R（+）形式的酯; （c）使（1）步骤（b）中获得的未反应的酯与三甲胺盐酸盐或（2）三甲胺反应，从而得到具有下式的酯：（Ⅳ）（d）水解该酯在步骤（c）中，在HCl存在下得到具有式（I）的L（ - ） - 肉碱氯化物。本发明还涉及包含3,4-环氧丁酸的酯的R（+）对映异构体的新一类化合物。

6. 发明授权

US5218130A 4-substituted anthracyclinones and their preparation 失效
标题翻译： 4-取代的蒽醌类化合物及其制备方法
公开(公告)号：US5218130A
公开(公告)日：1993-06-08
申请号：US646594
申请日：1991-01-25
申请人： Walter Cabri , Silvia De Bernardinis , Franco Francalanci , Sergio Penco
发明人： Walter Cabri , Silvia De Bernardinis , Franco Francalanci , Sergio Penco
IPC分类号： C07C49/337 , A45B23/00 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , C07C45/36 , C07C66/00 , C07C67/36 , C07C69/95 , C07H15/252
CPC分类号： C07H15/252
摘要： 4-substituted anthracyclinones of formula (I) ##STR1## wherein R represents a hydrogen atom or a straight or branched alkyl, alkenyl or alkynyl group having from 1 to 10 carbon atoms, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.

7. 发明授权

US5587495A 4-substituted anthracyclinones and anthracycline glycosides and the process for preparing them 失效
标题翻译： 4-取代的蒽环类抗生素和蒽环类苷及其制备方法
公开(公告)号：US5587495A
公开(公告)日：1996-12-24
申请号：US678352
申请日：1991-04-25
申请人： Walter Cabri , Silvia De Bernardinis , Franco Francalanci , Sergio Penco
发明人： Walter Cabri , Silvia De Bernardinis , Franco Francalanci , Sergio Penco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , B01J31/22 , C07B61/00 , C07C46/00 , C07C50/38 , C07C67/343 , C07C69/95 , C07F7/08 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： 4-substituted anthracyclinones of formula (I): ##STR1## wherein R represents a straight or branched alkyl, alkenyl or alkynyl group of up to 16 carbon atoms optionally substituted by (a) an aryl group which is unsubstituted or substituted by an inert group such as an alkyl, alkoxy or nitro group; (b) an alkoxy group; (c) a trialkylsilyl group, (d) an ester group or (e) an amido group, are intermediates in the preparation of antitumor anthracycline glycosides of formula (IX): ##STR2## wherein R is as defined above and R.sub.1 is a hydrogen atom or a hydroxy group, and pharmaceutically acceptable salts thereof.
摘要翻译： PCT No.PCT / EP89 / 01266 Sec。 371日期：1991年4月25日 102（e）日期1991年4月25日PCT提交1989年10月24日PCT公布。出版物WO90 / 04601 日期1990年5月3日，式（I）的取代的蒽环类：其中R表示直至16个碳原子的直链或支链烷基，烯基或炔基，任选被（a）芳基未取代或被惰性基团如烷基，烷氧基或硝基取代; （b）烷氧基; （c）三烷基甲硅烷基，（d）酯基或（e）酰胺基，是制备式（IX）的抗肿瘤蒽环类苷的中间体：其中R如上所定义，R 1 是氢原子或羟基，及其药学上可接受的盐。

8. 发明授权

US5180758A Process for preparing anthracyclinones 失效
标题翻译：制备蒽醌的方法
公开(公告)号：US5180758A
公开(公告)日：1993-01-19
申请号：US743373
申请日：1991-08-26
申请人： Walter Cabri , Ilaria Candiani , Silvia De Bernardinis , Franco Francalanci
发明人： Walter Cabri , Ilaria Candiani , Silvia De Bernardinis , Franco Francalanci
IPC分类号： B01J27/128 , B01J31/12 , C07B61/00 , C07C46/00 , C07C49/423 , C07C49/727 , C07C50/36 , C07C50/38
CPC分类号： C07C46/00 , Y02P20/55
摘要： 4-substituted anthracyclinones of general formula (I): ##STR1## wherein R represents a hydrogen atom or a COOR.sub.1 group in which R.sub.1 may be a hydrogen atom or an optionally substituted C.sub.1 -C.sub.10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by:(i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): ##STR2## wherein R' represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII):ML.sub.n L'.sub.m wherein M represents a transition metal atom, L and L', which may be the same or different, each represent an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII): ##STR3## wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R.sub.1 OH wherein R.sub.1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR.sub.1 group; and(ii) introducing an .alpha.-hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII).

9. 发明授权

US5103029A Process for preparing 4-demethoxydaunomycinone 失效
标题翻译：制备4-去甲基联苯胺的方法
公开(公告)号：US5103029A
公开(公告)日：1992-04-07
申请号：US333951
申请日：1989-04-06
申请人： Walter Cabri , Silvia de Bernardinis , Franco Francalanci , Sergio Penco
发明人： Walter Cabri , Silvia de Bernardinis , Franco Francalanci , Sergio Penco
IPC分类号： C07D317/26 , B01J31/02 , B01J31/24 , C07B61/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252
CPC分类号： C07C46/00 , Y02P20/55
摘要： 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.

10. 发明授权

US5015745A Process for the preparation of 4-demethoxydaunomycinone, the aglycone of 4-demethoxy-daunorubicin 失效
标题翻译： 4-脱甲氧基多霉素酮的制备方法，4-脱甲氧基柔红霉素的糖苷配基
公开(公告)号：US5015745A
公开(公告)日：1991-05-14
申请号：US306559
申请日：1989-02-06
申请人： Silvia De Bernardinis , Walter Cabri , Tiziano Martinengo , Franco Francalanci
发明人： Silvia De Bernardinis , Walter Cabri , Tiziano Martinengo , Franco Francalanci
IPC分类号： C07D317/20 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07C225/32 , C07C241/00 , C07C245/20 , C07D317/26 , C07D317/28 , C07H15/252
CPC分类号： C07C50/38 , C07C46/00 , C07C2103/46 , Y02P20/55
摘要： 4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyl-daunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound with an amine, removing the amino protecting group from the resultant 4-demethyl-4-(protected amino)-13-dioxolanyl-daunomycinone, diazotizing the thus-freed 4-amino group and reducing under mild conditions the resulting diazonium compound.

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