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1. 发明授权

US4170518A Microbiological conversion of sterol derivatives to 5-androsten-17-one derivatives and their use 失效
标题翻译：固醇衍生物微生物转化为5-雄酮-17-一种衍生物及其用途
公开(公告)号：US4170518A
公开(公告)日：1979-10-09
申请号：US710559
申请日：1976-07-30
申请人： Alfred Weber , Mario Kennecke , Alfred Popper , Rudolf Muller , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Gunter Neef , Rudolf Wiechert
发明人： Alfred Weber , Mario Kennecke , Alfred Popper , Rudolf Muller , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Gunter Neef , Rudolf Wiechert
IPC分类号： C12P33/16 , A61K31/5685 , C07J1/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J21/00 , C12P33/00 , C12R1/01 , C12R1/06 , C12R1/07 , C12R1/32 , C07B29/02
CPC分类号： C07J13/005 , C07J1/0011 , C07J1/0022 , C07J1/0037 , C07J1/0048 , C07J21/006 , C07J7/002 , C07J7/003 , C07J9/00 , C12P33/005
摘要： Sterol derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, or R.sub.1 and R.sub.2 collectively are lower alkylenedioxy and R.sub.3 is a sterol hydrocarbon side chain are converted to the corresponding androsten-17-ones by the oxidative degradation activity of a species of microorganism which degrades sterol side chains, preferably of the genus Mycobacterium. The ether group of those compounds wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, and the corresponding 17.beta.-hydroxy and 17.alpha.-hydrocarbon-17.beta.-hydroxy compounds is cleaved by reaction with an alkanoic acid chloride or anhydride in the presence of a Lewis acid.
摘要翻译：其中R 1是氢原子，R 2是低级烷氧基，或者R 1和R 2一起是低亚烷基二氧基并且R 3是一个固醇烃侧链的甾醇衍生物通过氧化降解被转化成相应的sten -17- 降解甾醇侧链，优选分枝杆菌属的微生物物种的活性。其中R 1为氢原子且R 2为低级烷氧基的那些化合物的醚基，并且相应的17β-羟基和17α-烃-17β-羟基化合物在存在下与链烷酰氯或酸酐反应而被裂解的路易斯酸。

2. 发明授权

US4024166A Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones 失效
标题翻译：制备13 {62-烷基-4-锑烯-3,17-二酮的方法
公开(公告)号：US4024166A
公开(公告)日：1977-05-17
申请号：US621384
申请日：1975-10-10
申请人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
发明人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
IPC分类号： B01J23/00 , C07B61/00 , C07C317/14 , C07D317/26 , C07D317/72 , C07J1/00
CPC分类号： C07C317/00 , C07D317/26 , C07D317/72 , C07J1/0059
摘要： Novel process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones of the formula ##STR1## wherein R.sub.1 is methyl or ethyl, consists of REACTING A 7A.beta.-ALKYL,5,6,7,7A-TETRAHYDROINDANE-1,5-DIONE WITH FORMALDEHYDE AND AN ARYLSULFINIC ACID OR AN ADDUCT OF FORMALDEHYDE AND ARYLSULFINIC ACID TO PRODUCE A TETRAHYDROINDANE DERIVATIVE;Hydrogenating the tetrahydroindane derivative with hydrogen in the presence of a palladium-, platinum-, or rhodium-containing hydrogenation catalyst to produce a perhydroindane derivative;Condensing the perhydroindane derivative in the presence of a proton-accepting agent with a 7,7-alkylenedioxy-3-oxooctanoic acid ester;Treating the product obtained with a strong aqueous base and then heating the product in an inert solvent to produce a 4,5-secosteroid;Hydrogenating the 4,5-secosteroid in the presence of a palladium-, platinum-, rhodium-, or nickel-containing hydrogenation catalyst; andHydrolyzing and cyclizing the hydrogenated 4,5-secosteroid by treatment with a strong acid.
摘要翻译：用于制备式“IMAGE”的13β-烷基-4-单宁-3,17-二酮的新方法，其中R 1是甲基或乙基，由反应A7Aβ-烷基，5,6,7,7a- 四氢呋喃-1,5-二酮与甲醛和氨基磺酸或甲醛和芳香酸的添加以生产四氢衍生物衍生物; 在含有氢氧化钯，或含氢氧化铑的氢化催化剂存在下氢化四氢呋喃衍生物生成四氢呋喃衍生物; 在具有7,7-亚甲基氧化亚硝酸酯酸酯的接受原料的情况下，冷凝该衍生物衍生物; 处理用强碱性基质获得的产品，然后加入产品中的产品用于生产4,5代谢物; 在含有钯，铑，铑，或含镍的氢化催化剂存在下氢化4,5-二氧化硫; 并通过用强酸处理氢化和循环氢化的4,5代谢物。

3. 发明授权

US4178381A C-homoestratrienes 失效
公开(公告)号：US4178381A
公开(公告)日：1979-12-11
申请号：US966162
申请日：1978-12-04
申请人： Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert , Yukishige Nishino , Gunter Neef
发明人： Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert , Yukishige Nishino , Gunter Neef
IPC分类号： C07J63/00 , C07J71/00 , A61K31/05 , A61K31/085 , A61K31/12
CPC分类号： C07J71/001 , C07J63/006 , C07J71/0005
摘要： C-homoestratrienes of the formula ##STR1## wherein ##STR2## R.sub.1 and R.sub.2 are the same or different, and each is hydrogen, acyl, alkyl, cycloalkyl or tetrahydropyranyl; andR.sub.3 is hydrogen, ethynyl or chloroethynyl; possess very good estrogenic properties.
摘要翻译：其中，R 1和R 2相同或不同，并且各自为氢，酰基，烷基，环烷基或四氢吡喃基; 并且R 3是氢，乙炔基或氯乙炔基; 具有非常好的雌激素特性。

4. 发明授权

US4155923A Process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives 失效
标题翻译：制备17 {62-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法
公开(公告)号：US4155923A
公开(公告)日：1979-05-22
申请号：US873444
申请日：1978-01-30
申请人： Gunter Neef , Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert
发明人： Gunter Neef , Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07J1/00 , C07J13/00 , C07J7/00
CPC分类号： C07J13/005 , C07J1/0033 , C07J13/007
摘要： A process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives of the formula ##STR1## WHEREIN R.sub.1 is methyl or ethyl;R.sub.2 is hydrogen or methyl, either being in the .alpha.-or .beta.-position;R.sub.3 is lower alkyl of 1-4 carbon atoms;R.sub.4 is alkyl of 1-8 carbon atoms or benzyl; andSt is the residue of a steroid ABC ring system;Comprises reacting (a) a 17-oxo compound of the formula ##STR2## WHEREIN R.sub.1 and R.sub.2 are as defined above andSt* is said steroid ABC ring system residue, St, in a form which is chemically compatible with said reaction;With (b) an enolate ion of an alkoxyacetic acid alkyl ester of the formula ##STR3## wherein R.sub.3 and R.sub.4 are as defined above.
摘要翻译：制备式Ia的17β-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法，其中R1是甲基或乙基; R2是氢或甲基，或者是α位或β-位; R3是1-4个碳原子的低级烷基; R4是1-8个碳原子的烷基或苄基; St是类固醇ABC环系统的残基; 包含反应（A）制剂的17-OXO化合物，其中R1和R2如上所定义，St *是所述类固醇ABC环系统残基St，以与所述反应化学相容的形式; 具有（B）式（A）的化合物，其中R 3和R 4如上所定义的烷氧基酸酯。

5. 发明授权

US4077996A Process for the preparation of trans-deca hydronaphthalene derivatives 失效
标题翻译：反十氢化萘衍生物的制备方法
公开(公告)号：US4077996A
公开(公告)日：1978-03-07
申请号：US676805
申请日：1976-04-14
申请人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
发明人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
IPC分类号： C07C69/013 , C07C45/00 , C07C49/385 , C07C49/517 , C07C49/753 , C07C67/00 , C07C69/66 , C07C253/00 , C07C255/31 , C07D317/50 , C07D317/72 , C07D321/00 , C07F7/18 , C07C120/00 , C07C121/46 , C07D319/02 , C07D319/04
CPC分类号： C07F7/1856 , C07D317/50
摘要： A process for the preparation of trans-decahydronaphthalene compounds of Formula I ##STR1## wherein X is lower alkyl, --(CH.sub.2).sub.3 --Z--R.sub.2, ##STR2## --(CH.sub.2).sub.3 COOR.sub.4, or --(CH.sub.2).sub.3 CN; Y and Z are ketalized carbonyl or free, esterified, or etherified hydroxymethylene;U is halogen;R.sub.1, r.sub.2, and R.sub.3 are lower alkyl; andR.sub.4 is alkyl;Wherein an octahydronaphthalene compound of Formula II ##STR3## is converted, in the presence of bases, by reaction of a trialkyl chlorosilane of the formula(R.sub.5).sub.3 Si--Clwherein the R.sub.5 each are lower alkyl group, to a hexahydronaphthalene compound of the formula ##STR4## The hexahydronaphthalene compound is hydrogenated, in an inert solvent with hydrogen in the presence of a platinum-, palladium-, or rhodium-containing hydrogenation catalyst, to an octahydronaphthalene compound of the formula ##STR5## and a vinyl ketone of the formulaXCOCH.dbd.CH.sub.2is added to the thus-obtained octahydronaphthalene compound in an inert solvent in the presence of a Lewis acid.
摘要翻译：制备式I的反十氢萘化合物的方法，其中X是低级烷基， - （CH 2）3 -Z-R 2， - （CH 2）3 COOR 4或 - （CH 2）3 C 3; Y和Z是缩酮化羰基或游离的，酯化的或醚化的羟基亚甲基; U是卤素; R1，R2和R3是低级烷基; 和R4是烷基; 在碱的存在下，通过式（R5）3Si-Cl的三烷基氯硅烷与各自为低级烷基的R 5反应得到式II的六氢萘化合物，其中式II的甲氧基二苯甲酮化合物转化为式VI化合物在惰性溶剂中，在含有铂，钯或铑的氢化催化剂的存在下，用氢气将其氢化成式为“八氢”的八氢化合物和式在路易斯酸存在下，在惰性溶剂中将式XCOCH = CH 2加入到如此获得的八氢萘化合物中。

6. 发明授权

US4333928A 16 .alpha.-Alkyl steroids, their preparation, and pharmaceutical preparations thereof 失效
标题翻译： 16α-烷基甾类，它们的制备及其药物制剂
公开(公告)号：US4333928A
公开(公告)日：1982-06-08
申请号：US150518
申请日：1980-05-16
申请人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Rudolf Wiechert , Hermann Steinbeck
发明人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Rudolf Wiechert , Hermann Steinbeck
IPC分类号： A61K31/565 , A61K31/58 , C07J1/00 , C07J17/00 , C07J41/00 , A61K31/56
CPC分类号： C07J1/0096 , C07J1/0059 , C07J1/007 , C07J17/00 , C07J41/0005 , C07J41/0088
摘要： 16 .alpha.-Alkyl steroids of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, alkyl, acyl, or glycosylR.sub.3 is hydrogen or a substituted or unsubstituted, saturated or unsaturated lower hydrocarbon residue, andR.sub.4 is methyl, ethyl or propyl, exhibit strong progestational activity and a very low androgenic activity.
摘要翻译： 16α-烷基甾族化合物，其中R1是氢或甲基，R2是氢，烷基，酰基或糖基R3是氢或取代或未取代的饱和或不饱和低级烃基，R4是甲基，乙基或丙基，表现出强烈的促孕活性和非常低的雄激素活性。

7. 发明授权

US4012420A 9,10-Secoestrane derivatives and their production 失效
标题翻译： 9,10-Secoestrane衍生物及其生产
公开(公告)号：US4012420A
公开(公告)日：1977-03-15
申请号：US570072
申请日：1975-04-21
申请人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
发明人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07C49/84 , C07C69/01 , C07C401/00 , C07D317/46 , C07D319/08
CPC分类号： C07D317/46 , C07C49/84 , C07C69/01
摘要： 9,10-Secoestranes, useful as intermediates in the total synthesis of steroids, of the formula ##STR1## WHEREIN N IS 1 OR 2, R.sub.1 is lower alkyl, R.sub.2, R.sub.3 and R.sub.4 are hydrogen, alkoxy or acyloxy, X is free or ketalized carbonyl or free, esterified or etherified hydroxymethylene, and Y is carbonyl or dialkoxymethylene are produced by condensing, in the presence of a basic catalyst, ##STR2## WHEREIN X, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4 have the values given above, and Z is Cl, Br or I, to produce a 9,10-secoestrane of the above formula wherein Y is a free carbonyl group, which can then, if desired, be ketalized to a corresponding compound wherein Y is dialkoxymethylene or like ketal group.
摘要翻译： 9,10-Secoestranes，用作类固醇总合成中的中间体，式为“IMAGE”，其中N为1或2，R 1为低级烷基，R 2，R 3和R 4为氢，烷氧基或酰氧基，X为游离或缩酮化的羰基或游离的，酯化的或醚化的羟基亚甲基，Y是羰基或二烷氧基亚甲基，是在碱性催化剂存在下，通过在上述给定的值下，并且Z是Cl，Br或I，以产生上式的9,10-隔离子，其中Y是游离羰基，如果需要，其可以被缩醛化成相应的化合物，其中Y是二烷氧基亚甲基或类似的缩酮基。

8. 发明授权

US4202991A Novel bicycloalkane derivatives and the production thereof 失效
标题翻译：新型双环烷烃衍生物及其制备方法
公开(公告)号：US4202991A
公开(公告)日：1980-05-13
申请号：US753996
申请日：1976-12-27
申请人： Gerhard Sauer , Helmut Hauser , Gregor Haffer , Juergen Ruppert , Ulrich Eder , Rudolf Wiechert
发明人： Gerhard Sauer , Helmut Hauser , Gregor Haffer , Juergen Ruppert , Ulrich Eder , Rudolf Wiechert
IPC分类号： C07C317/00 , C07D317/30 , C07D317/46 , C07D319/06 , C07C69/145 , C07C69/24
CPC分类号： C07D319/06 , C07C317/00 , C07C321/00 , C07D317/30 , C07D317/46
摘要： Bicycloalkane derivatives of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is lower alkyl, Acyl is alkanoyl, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is alkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is acyl or phenyl optionally substituted with lower alkoxy, benzyloxy or alkanoyloxy; and Z is nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or sulfinic acid, followed if desired by oxidation and optional salt condensation.
摘要翻译：其中n为1或2，R 1为低级烷基，酰基为烷酰基，Y为-S-R 2，-SO m -R 2或者其中m为1或2，R 2为烷基，R 3是氢或低级烷基，R 4是任选被低级烷氧基，苄氧基或烷酰氧基取代的酰基或苯基; Z是硝基，低级烷氧基羰基，低级烷酰基，低级烷基亚磺酰基或低级烷基磺酰基是类固醇总合成中的有用中间体。通过使缺少CH 2 Y取代基的相应化合物与甲醛和硫醇或亚磺酸反应制备化合物，随后如果需要，通过氧化和任选的盐缩合。

9. 发明授权

US4032540A Benzopyran derivatives 失效
标题翻译： BENZOPYRAN衍生物
公开(公告)号：US4032540A
公开(公告)日：1977-06-28
申请号：US664316
申请日：1976-03-05
申请人： Ulrich Eder , Gerhard Sauer , Gregor Haffer , Jurgen Ruppert , Rudolf Wiechert
发明人： Ulrich Eder , Gerhard Sauer , Gregor Haffer , Jurgen Ruppert , Rudolf Wiechert
IPC分类号： C07D317/44
CPC分类号： C07D317/44
摘要： Benzopyran derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.3 each are lower alkyl; n is the integer 1 or 2; --A--B-- is >CH--CH.sub.2 - or >CH=CH-; X is a free, esterified or etherified hydroxy group; and Y is H or X and Y collectively are =O; and W is --(CH.sub.2).sub.3 --Z--R.sub.4 ##STR2## --(CH.sub.2).sub.3 --COOR.sub.6 or --(CH.sub.2).sub.3 CN, wherein V is halogen, Z is a ketalized carbonyl group or a free, esterified or etherified hydroxymethylene group; R.sub.4 and R.sub.5 each are lower alkyl and R.sub.6 is alkyl, aryl or aralkyl, are valuable intermediates in the synthesis of steroids.

10. 发明授权

US3976701A Process for the preparation of 9,10-secoestrane derivatives 失效
标题翻译：制备9,10-secoestrane衍生物的方法
公开(公告)号：US3976701A
公开(公告)日：1976-08-24
申请号：US409234
申请日：1973-10-24
申请人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
发明人： Ulrich Eder , Gregor Haffer , Jurgen Ruppert , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07C69/16 , B01J27/00 , B01J31/00 , C07B61/00 , C07C27/00 , C07C29/132 , C07C29/136 , C07C35/23 , C07C41/00 , C07C43/168 , C07C43/178 , C07C43/18 , C07C43/196 , C07C43/20 , C07C43/23 , C07C45/00 , C07C49/675 , C07C49/84 , C07C67/00 , C07D307/77 , C07D319/08 , C07J1/00 , C07J51/00
CPC分类号： C07D307/77 , C07C43/168 , C07C43/20 , C07J1/00 , C07J51/00
摘要： 6,9-Oxido-9,10-seco-1,3,5(10),6,8,14-estrahexaenes, useful as intermediates in the total synthesis of steroids, of the formula ##SPC1##Wherein n is 1 or 2, R.sub.1 is lower-alkyl, R.sub.2, R.sub. 3 and R.sub.4 are H, alkoxy or acyloxy, X is a free or ketalized keto or free, esterified or etherified hydroxymethylene, are produced by the cyclization, with an acid catalyst, of a 9,10-secoestrane of the formula ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and n have the values given above, and Q is carbonyl or dialkoxymethylene. Hydrogenation produces the corresponding 6,9-oxido-9,10-seco-1,3,5(10)-estratrienes and 9-oxy-9,10-seco-1,3,5(10)-estratrienes.
摘要翻译： 6,9-氧代-9,10-断-1,3,5（10），6,8,14-异己烯，其用作全合成类固醇的中间体，式为WHEREIN N IS 1 OR 2，R1 是低级烷基，R 2，R 3和R 4是H，烷氧基或酰氧基，X是游离或缩酮化酮或游离的酯化或醚化的羟基亚甲基，通过酸催化剂与9,10- 式WHEREIN R1，R2，R3，R4，X和n具有上面给出的值，Q是羰基或二烷氧基亚甲基。氢化产生相应的6,9-氧化-9,10-断-1,3,5（10） - 三亚甲基和9-氧基-9,10-断-1,3,5（10） - 三亚甲基。

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