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1. 发明专利

AU778887B2 A new process for the preparation of latanoprost 未知
公开(公告)号：AU778887B2
公开(公告)日：2004-12-23
申请号：AU2878101
申请日：2001-01-26
申请人： FINETECH LAB LTD
发明人： GUTMAN ARIE , NISNEVICH GENNADIY , ETINGER MARINA , ZALTZMAN IGOR , JUDOVICH LEV , PERTSIKOV BORIS
IPC分类号： C07D307/935 , A61K31/5575 , A61P43/00 , C07B61/00 , C07C405/00 , C07D309/12 , C07D407/12 , A61K31/557
摘要： Disclosed is a process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.

2. 发明专利

HU0204395A2 A NEW PROCESS FOR THE PREPARATION OF LATANOPROST 未知
公开(公告)号：HU0204395A2
公开(公告)日：2003-04-28
申请号：HU0204395
申请日：2001-01-26
申请人： FINETECH LAB LTD
发明人： ETINGER MARINA , GUTMAN ARIE , JUDOVICH LEV , NISNEVICH GENNADIY , PERTSIKOV BORIS , ZALTZMAN IGOR
IPC分类号： C07D307/935 , A61K31/5575 , A61P43/00 , C07B61/00 , C07C405/00 , C07D309/12 , C07D407/12
摘要： Disclosed is a process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.

3. 发明专利

HU0303557A2 PROCESS AND INTERMEDIATES FOR PRODUCTION OF CABERGOLINE AND RELATED COMPOUNDS 未知
公开(公告)号：HU0303557A2
公开(公告)日：2004-03-01
申请号：HU0303557
申请日：2001-04-16
申请人： FINETECH LAB LTD
发明人： GUTMAN ARIE L , NISNEVICH GENNADIY , PERTSIKOV BORIS , RUKHMAN IGOR , TISHIN BORIS , VILENSKY ALEX
IPC分类号： C07B61/00 , C07D457/06 , C07F7/10

4. 发明专利

CZ20024100A3 Process and intermediates for preparing cabergoline and related compounds 未知
公开(公告)号：CZ20024100A3
公开(公告)日：2003-10-15
申请号：CZ20024100
申请日：2001-04-16
申请人： FINETECH LAB LTD
发明人： GUTMAN ARIE L , NISNEVICH GENNADIY , RUKHMAN IGOR , TISHIN BORIS , VILENSKY ALEX , PERTSIKOV BORIS
IPC分类号： C07D457/06

5. 发明专利

CA2412861A1 PROCESS AND INTERMEDIATES FOR PRODUCTION OF CABERGOLINE AND RELATED COMPOUNDS 未知
公开(公告)号：CA2412861A1
公开(公告)日：2002-10-31
申请号：CA2412861
申请日：2001-04-16
申请人： FINETECH LAB LTD
发明人： GUTMAN ARIE L , NISNEVICH GENNADIY , PERTSIKOV BORIS , TISHIN BORIS , RUKHMAN IGOR , VILENSKY ALEX
IPC分类号： C07B61/00 , C07D457/06 , C07F7/10
摘要： A process for preparation of N-(ergoline-8.beta.-carbonyl)ureas of the formula [I] their stereoisomers as well as acid addition salts thereof which process comprises silylating an ergoline -8.beta.-carboxamide of the formula [2], their stereoisomers as well as metal or ammonium salts or acid addition salts thereof and reacting the resultant product with an isocyanates R1N=C=O [5] wherein R1 is selected from alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, and dimethylamino alkyl group -(CH2)nNMe2 in which n is an integer, R2 is selected from hydrogen, alkyl having from 1 to 4 carbon atoms , cyclohexyl, phenyl, dimethylamino alkyl group -(CH2)nNMe2 in which n is an integer, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl or thiadiazol yl , R3 represents a hydrocarbon group having from 1 to 4 carbon atoms, and R4 is selected from hydrogen, halogen, methylthio and phenylthio group; followed b y desilylation. This novel approach provides an efficient method for preparati on of N-(ergoline-8.beta.-carbonyl)ureas of the formula [I] which can be useful as anty-Parkinson drugs and prolactin inhibitors. One of the most potent antiprolactinic agent of the class of compounds prepared according to the present invention is Cabergoline. Silylated ergolines, which are obtaine d as intermediates in the process of the present invention, are novel compound s and represent a further aspect of the invention.

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