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1. 发明专利

HU0500817A2 ENVIRONMENT-FRIENDLY PROCESS FOR THE SYNTHESIS OF QUATERNARY AMINO-STEROIDS 未知
公开(公告)号：HU0500817A2
公开(公告)日：2006-05-29
申请号：HU0500817
申请日：2005-09-02
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN DR , MAHO SANDOR , SZABO GYOERGYI , GALIK GYOERGY DR , BALOGH GABOR
IPC分类号： C07J43/00

2. 发明专利

HU224816B1 PROCESS FOR PRODUCING A-NOR-SECO-STEROIDE COMPOUNDS, SECO-INDOXYLIDENECARBOXILICACID DERIVETIVES AS INTERMEDIATES THEREOF 未知
公开(公告)号：HU224816B1
公开(公告)日：2006-02-28
申请号：HU9901939
申请日：1999-06-10
申请人： RICHTER GEDEON VEGYESZET
发明人： SANTA CSABA , MAHO SANDOR , TUBA ZOLTAN DR , SZILAGYI GABRIELLA , BAKCSI ERIKA , SZELES JANOS , BALOGH GABOR , BRLIK JANOS , TRISCHLER FERENC DR
IPC分类号： C07C62/06 , C07C51/285 , C07D209/36
摘要： The invention relates to a new process for the synthesis of 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-3-acid derivatives of formula (I)wherein the meaning of Z is carboxyl or formyl group andto the new secoindoxylidene carboxylic acid derivatives of formula (II)wherein R1 and R2 independently are C1-C4 alkyl or alkoxy group, hydrogen or halogen atom-which are intermediates for preparing the compounds of formula (I).The 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one), which is used as anabolic in therapy.

3. 发明专利

AT364096B 未知
公开(公告)号：AT364096B
公开(公告)日：1981-09-25
申请号：AT597078
申请日：1978-08-17
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN DR , MARSAI MARIA DIPL ING , GOEROEG SANDOR DR , BIRO KATALIN DR , KARPATI EGON DR , SZPORNY LASZLO DR
IPC分类号： C07D221/18 , A61K31/395 , A61P21/02 , C07J73/00

4. 发明专利

AU1612476A TRIAMINO-ANDROSTANES 未知
公开(公告)号：AU1612476A
公开(公告)日：1978-01-26
申请号：AU1612476
申请日：1976-07-22
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN DR , MARSAI MARIA , BIRO KATALIN , SZPORNY LASZLO DR , KARPATI EGON DR , SZEBERENYI SZABOLCS DR
IPC分类号： C07J1/00 , A61K31/565 , A61K31/569 , A61K31/58 , A61P21/02 , C07J11/00 , C07J13/00 , C07J41/00 , C07J43/00 , C07J71/00

5. 发明专利

DE2130280A1 未知
公开(公告)号：DE2130280A1
公开(公告)日：1971-12-23
申请号：DE2130280
申请日：1971-06-18
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN DR , GEB SZABO MARIA BOR
IPC分类号： C07J9/00 , C07D221/18 , C07J73/00 , C07D101/00
摘要： A process for the preparation of cholestane derivatives and their salts, which contain a nitrogen atom in position 2 or 3 of the general formula i ** (see formula) ** Wherein a and b represent carbonyl, methylene, imino or N-methylimino groups, with the restriction that, within the same compound, a and b are different, but a or b always represent an imino, or N-methylimino, group by the fact that a compound of the general formula ii ** (see formula) ** Wherein x and y represent a carbamoyl and/or carbomethoxy or carboethoxy group, but in at least one compound, it is reacted with lead tetraacetate and then the compound thus formed is subjected to a ring closure reaction in the presence of a alkali metal hydroxide or an alkali metal alcoholate and then, if desired, the lactams of the general formula i are subjected: a) to methylation with methyl iodide in the presence of potassium tert-butylate and, if required, to reduction with sodium hydride-bis- (2-methoxy-ethoxy) -aluminium; or b) reduction with a complex metal hydride, and subsequent methylation with formaldehyde in a formic acid medium and, if desired, the salt of the base thus obtained is formed. (Machine-translation by Google Translate, not legally binding)

7. 发明专利

HU224817B1 NEW PROCESS FOR PRODUCING 17-BETHA-HYDROXY-17-ALPHA-METHYL-2-OXA-5-ALPHA-ANDROSTAN-3-ON AND INTERMEDIATE THEREOF 未知
公开(公告)号：HU224817B1
公开(公告)日：2006-02-28
申请号：HU9901938
申请日：1999-06-10
申请人： RICHTER GEDEON VEGYESZET
发明人： SANTA CSABA , MAHO SANDOR , TUBA ZOLTAN DR , MESTER TAMAS , TROMPLER ARPAD , SZELES JANOS , LANCOS KRISZTINA DR , FERENCZINE DR FODOR KATALIN , HORVATH PETER DR
IPC分类号： C07J75/00 , C07J73/00
摘要： The invention relates to a new process for the synthesis of 17beta-hydroxy-17alpha-methyl-2-oxa-5alpha-androstane-3-one of formula (I). The process according to the invention is as follows: the 17beta-hydroxy-17alpha-ethyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid of formula (III) is transformed into the ring-closed 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) in an inert solvent or without solvent with a C2-C3 alkan acid anhydride or a substituted carbodiimide of formula R1-N=C=N-R2- wherein R1 and R2 independently are C1-C6 alkyl group, C1-C6 alkyl group substituted by tertiary or quaternary amino group or 1-3 phenyl group, C5-C6 cycloalkyl group, aryl group substituted by 1-3 methoxy, tertiary amino, nitro, C1-C4 alkyl group or 1-3 halogen atom-and the obtained compound of formula (II) is reduced regioselectively by a complex alkali metal hydride in an inert solvent The new 17beta-hydroxy-17alpha-methyl-1,3-seco-2-nor-5alpha-androstane-1,3-diacid anhydride of formula (II) is also the subject of the invention.

8. 发明专利

AU5239700A Process for the synthesis of n-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenyl-sulfonyl)-2-hydroxy-2-methyl-propionamide 未知
公开(公告)号：AU5239700A
公开(公告)日：2001-01-31
申请号：AU5239700
申请日：2000-05-26
申请人： RICHTER GEDEON VEGYESZET
发明人： SOROS BELA , TUBA ZOLTAN DR , GALIK GYORGY , BOR ADAM , DEMETER ADAM , TRISCHLER FERENC , HORVATH JANOS , BRLIK JANOS
IPC分类号： C07C253/30 , C07C255/60 , C07C303/28 , C07C309/66 , C07C315/02 , C07C317/46 , C07C319/14 , C07C323/60 , C07D327/10
摘要： A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.

9. 发明专利

AU4352693A Novel process for preparing 17beta -substituted 4-azaandrostane derivatives 未知
公开(公告)号：AU4352693A
公开(公告)日：1995-01-17
申请号：AU4352693
申请日：1993-06-24
申请人： RICHTER GEDEON VEGYESZET
发明人： TUBA ZOLTAN DR , HORVATH JUDIT DR , SZELES JANOS , KOLLAR LASZLO , BALOGH GABOR
IPC分类号： A61K31/58 , A61P43/00 , C07J20060101 , C07J73/00
摘要： The invention relates to a novel process for preparing 17 beta -substituted 4-azaandrostane derivatives of general formula (I) wherein R represents hydrogen or a C1-3alkyl group; R represents a carboxamido group mono- or disubstituted by C1-8alkyl group(s); or a free carboxyl group; or a carboxyl group esterified with a C1-5 alcohol; and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line represents a single or double bond; as well as their salts. The process comprises reacting a 17-halogeno-4-azaandrostene derivative of general formula (II) wherein R and the - &cir& _- &cir& _- &cir& _- &cir& _ bond line are as defined above, and X is chlorine, bromine or iodine, with a primary or secondary alkylamine or a C1-5 alcohol, in dimethylformamide or dimethylsulfoxide medium in the presence of a palladium(II) salt and phosphines or a palladium(II) complex and a tertiary amine base in carbon monoxide atmosphere at a temperature between 35 DEG C and 80 DEG C, then, if desired, transforming an obtained compound of general formula (I) to another compound of general formula (I) by hydrogenation, hydrolysis or salt forming reaction.

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