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1. 发明授权

US4133826A Novel inversion process 失效
标题翻译：新型反演过程
公开(公告)号：US4133826A
公开(公告)日：1979-01-09
申请号：US789774
申请日：1977-04-22
申请人： Julien Warnant , Jacques Marechal-Prost , Philippe Cosquer
发明人： Julien Warnant , Jacques Marechal-Prost , Philippe Cosquer
IPC分类号： A01N37/34 , A01N53/00 , A01N53/08 , A01N53/14 , A01P7/04 , A61K31/135 , A61K31/33 , A61K31/395 , A61K31/545 , C07B31/00 , C07B55/00 , C07B57/00 , C07C67/00 , C07C69/74 , C07C69/743 , C07C69/747 , C07C217/30 , C07C233/25 , C07C235/46 , C07C253/00 , C07C253/30 , C07C255/32 , C07C255/38 , C07C255/39 , C07C255/53 , C07C313/00 , C07C319/20 , C07C323/20 , C07D213/62 , C07D213/63 , C07D213/64 , C07D213/69 , C07D213/75 , C07D213/81 , C07D213/82 , C07D233/70 , C07D239/32 , C07D239/34 , C07D241/18 , C07D317/64 , C07D501/06 , C07C121/75
CPC分类号： C07C255/00 , A01N53/00 , C07C255/53
摘要： A process for the preparation of an ester of chiral (A) acid with an optically active (S) .alpha.-cyano-3-phenoxybenzyl alcohol by reacting an ester of chiral (A) acid with .alpha.-cyano-3-phenoxybenzyl alcohol of the formula ##STR1## in its optically active (R) form or a racemic (R,S) mixture or a mixture of esters of said (R) alcohol and (S) alcohol in non-equimolecular proportions designated herein as "ester (R+S)" with a base selected from the group consisting of ammonium hydroxide, primary, secondary and tertiary amines, quaternary ammonium compounds, liquid amines of high molecular weight, ion exchange resins of a basic character and a catalytic amount of a strong base in at least one solvent in which the ester of the (R) alcohol is soluble and in which the ester of the (S) alcohol is insoluble and recovering from the resulting medium the chiral (A) acid ester of the (S) alcohol which is insoluble.
摘要翻译：通过使手性（A）酸的酯与α-氰基-3-苯氧基苄醇的酯反应，由手性（A）酸与光学活性（S）α-氰基-3-苯氧基苄基醇的酯的制备方法式（B）其光学活性（R）形式的式（B）或外消旋（R，S）混合物或所述（R）醇和（S）醇的酯的混合物以本文称为“酯 + S）“，碱选自氢氧化铵，伯，仲和叔胺，季铵化合物，高分子量的液胺，基本特征的离子交换树脂和催化量的强碱至少一种溶剂，其中（R）醇的酯可溶，并且其中（S）醇的酯不溶于其中并从所得介质中回收（S）醇的手性（A）酸酯，其为不溶。

2. 发明授权

US4190658A 14-Imino-(15H)-eburnamine compounds, compositions, methods of use and process of synthesis 失效
标题翻译： 14-Imino-（15H） - 乙二胺化合物，组合物，使用方法和合成方法
公开(公告)号：US4190658A
公开(公告)日：1980-02-26
申请号：US925103
申请日：1978-07-17
申请人： Julien Warnant , Andre Farcilli , Italo Medici
发明人： Julien Warnant , Andre Farcilli , Italo Medici
IPC分类号： C07D461/00 , A61K31/475 , C07D471/22
CPC分类号： C07D461/00
摘要： Novel eburnamenine derivatives of the formula ##STR1## in the form of racemic mixtures or optically active isomers and their non-toxic, pharmaceutically acceptable acid addition salts which are oxygenators and cerebral vasoregulators of great value.
摘要翻译：新型的具有外消旋混合物或光学活性异构体形式的本发明的伊本那米衍生物及其无毒的药学上可接受的酸加成盐，它们是具有重要价值的氧合器和脑血管调节剂。

3. 发明授权

US4136195A Insecticidal cyclopropane carboxylates 失效
标题翻译：杀虫环孢菌素羧酸酯
公开(公告)号：US4136195A
公开(公告)日：1979-01-23
申请号：US789842
申请日：1977-04-22
申请人： Julien Warnant , Jacques Prost-Marechal , Philippe Cosquer
发明人： Julien Warnant , Jacques Prost-Marechal , Philippe Cosquer
IPC分类号： A01N37/34 , A01N53/00 , A01N53/08 , A01N53/14 , A01P7/04 , A61K31/135 , A61K31/33 , A61K31/395 , A61K31/545 , C07B31/00 , C07B55/00 , C07B57/00 , C07C67/00 , C07C69/74 , C07C69/743 , C07C69/747 , C07C217/30 , C07C233/25 , C07C235/46 , C07C253/00 , C07C253/30 , C07C255/32 , C07C255/38 , C07C255/39 , C07C255/53 , C07C313/00 , C07C319/20 , C07C323/20 , C07D213/62 , C07D213/63 , C07D213/64 , C07D213/69 , C07D213/75 , C07D213/81 , C07D213/82 , C07D233/70 , C07D239/32 , C07D239/34 , C07D241/18 , C07D317/64 , C07D501/06 , A01N9/20 , C07C121/66
CPC分类号： C07C255/00 , A01N53/00 , C07C255/53
摘要： The novel esters, (R) .alpha.-cyano-3-phenoxybenzyl 2,2-dimethyl-3R-(2,2-dichlorovinyl)-cyclopropane-1R-carboxylate and (S) .alpha.-cyano-3-phenoxybenzyl 2,2-dimethyl-3R-(2,2-dichlorovinyl)-cyclopropane-1R-carboxylate, having insecticidal properties.

4. 发明授权

US4277409A Preparation of 9.alpha.-fluoro-16.alpha.-methyl-21-acetoxy-.DELTA..sup.1,4 -pregnadiene-11.beta.-ol-3,20-dione 失效
标题翻译： 9α-氟-16α-甲基-21-乙酰氧基-TATA 1,4-孕甾二烯-11β-醇-3,20-二酮的制备
公开(公告)号：US4277409A
公开(公告)日：1981-07-07
申请号：US94772
申请日：1979-11-16
申请人： Julien Warnant , Jean Jolly
发明人： Julien Warnant , Jean Jolly
IPC分类号： C07J5/00 , C07J13/00
CPC分类号： C07J5/0038 , C07J13/005
摘要： An improved process for the preparation of pure 9.alpha.-fluoro-16.alpha.-methyl-21-acetoxy-.DELTA..sup.1,4 -pregnadiene-11.beta.-ol-3,20-dione comprising reacting 9.alpha.-fluoro-21-acetoxy-.DELTA..sup.1,4,16 -pregnatriene-11.beta.-ol-3,20-dione with a methyl magnesium halide in the presence of a catalytic amount of a cuprous halide effecting protonation of magnesian to form 9.alpha.-fluoro-16.alpha.-methyl-21-acetoxy-.DELTA..sup.1,4 -pregnadiene-11.beta.-ol-3,20-dione, reacting the raw product with an acetylation agent to acetylate the partially deacetylated product and purifying the reacetylated product with an organic solvent, treating in solution with a peroxidation agent and then purifying again with an organic solvent.
摘要翻译：制备纯的9α-氟-16α-甲基-21-乙酰氧基-TATA-孕烯二烯-11β-醇-3,20-二酮的改进方法，包括使9α-氟-21-乙酰氧基-D- DELTA 1,4,16-孕三烯-11β-醇-3,20-二酮与甲基卤化镁在催化量的卤化亚铜存在下进行质子化的氧化镁，形成9α-氟-16α-甲基 -21-乙酰氧基-DDTA 1,4-孕甾二烯-11β-醇-3,20-二酮，使原料与乙酰化反应物乙酰化部分脱乙酰化产物并用有机溶剂纯化再乙酰化产物，在溶液中处理用过氧化剂再次用有机溶剂纯化。

5. 发明授权

US4186128A Novel process for the preparation of 3-oximes of steroids 失效
标题翻译：用于制备3-肟类固醇的新方法
公开(公告)号：US4186128A
公开(公告)日：1980-01-29
申请号：US926865
申请日：1978-07-24
申请人： Julien Warnant , Jean Jolly
发明人： Julien Warnant , Jean Jolly
IPC分类号： C07D317/72 , C07J41/00 , C07J43/00 , C07J1/00
CPC分类号： C07D317/72 , C07J41/0016 , C07J43/003 , C07C2103/16
摘要： A novel process for the preparation of 3-oximes of the formula ##STR1## wherein R is selected from the group consisting of methyl and ethyl and R' is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 2 to 8 carbon atoms and novel intermediates formed therein.
摘要翻译：一种用于制备式I的3-肟的新方法，其中R选自甲基和乙基，R'选自氢和有机羧酸的酰基2至 8个碳原子和其中形成的新型中间体。

6. 发明授权

US3980687A Intermediates for the preparation of 17-substituted-.DELTA..sup.4 -gonenes 失效
标题翻译：用于制备17-取代的{66 {hu 4 {b-蒎烯
公开(公告)号：US3980687A
公开(公告)日：1976-09-14
申请号：US489616
申请日：1974-07-18
申请人： Julien Warnant , Jean Jolly , Robert Joly
发明人： Julien Warnant , Jean Jolly , Robert Joly
IPC分类号： A41B1/00 , A41B3/00 , C07J1/00 , C07J7/00 , C07J41/00 , C07J73/00 , C07J75/00 , C07C69/145 , C07C69/24 , C07C69/61 , C07C69/74
CPC分类号： C07J73/00 , C07J1/00 , C07J41/00 , C07J7/00 , C07J75/00
摘要： A process for the production of a .DELTA..sup.4 -gonenic steroid having the formula ##SPC1##Wherein R represents a member selected from the group consisting of hydrogen and the acyl of an organic carboxylic acid having from 1 to 18 carbon atoms, R' represents an alkyl having from 1 to 4 carbon atoms, R.sup.iv represents a member selected from the group consisting of lower alkyl, lower alkenyl or lower alkynyl, and B represents a member selected from the group consisting of two hydrogens in the 9.alpha. and 10.beta. position and a double bond which comprises the steps of reacting a 3-ketal-4,5-seco-gonane-5-one with a ketalizing agent, oxidizing the resultant 3,5-diketal-4,5-seco-gonane-17.beta.-ol, reacting the resultant 3,5-diketal-4,5-seco-gonane-17-one with an organometallic compound, hydrolyzing the resultant 3,5-diketal-17.alpha.-R.sup.iv -4,5-seco-gonane-17.beta.-ol, cyclizing the resultant 17.alpha.-R.sup.iv -4,5-seco-gonane-17.beta.-ol-3,5-dione and recovering said .DELTA..sup.4 -gonenic steroid. The novel intermediates are also part of the invention. The .DELTA..sup.4 -gonenic steroids are known compounds having steroidal properties.
摘要翻译：一种制备具有式WHEREIN R的一种DELTA 4-型类固醇的方法，其选自氢和具有1至18个碳原子的有机羧酸的酰基，R'表示具有 1至4个碳原子，Riv表示选自低级烷基，低级烯基或低级炔基的成员，B表示选自9α和10β位中的两个氢和双键的成员其包括使3-缩酮-4,5-二羟基喹啉-5-酮与缩酮剂反应的步骤，将所得3,5-二缩酮-4,5-二羟基-17β-醇氧化，使所得的3,5-二缩酮-4,5-二缩酮-17-酮与有机金属化合物，水解所得的3,5-二缩酮-17α-1R-4,5-间苯二酚-17β-醇，使得到的17α-Riv-4,5-Seco-gonane-17β-羟基-3,5-二酮环化并回收所述DELTA4-型葡萄糖甾族化合物。新颖的中间体也是本发明的一部分。 DELTA 4-Gonenic类固醇是具有甾体特性的已知化合物。

7. 发明授权

US3974182A Intermediates for the preparation of trienic steroids 失效
标题翻译：用于制备三烯类固醇的中间体
公开(公告)号：US3974182A
公开(公告)日：1976-08-10
申请号：US590267
申请日：1975-06-25
申请人： Julien Warnant , Jean Jolly
发明人： Julien Warnant , Jean Jolly
IPC分类号： C07J1/00 , C07J75/00 , C07D317/72
CPC分类号： C07J1/00 , C07J75/00 , C07C2103/16
摘要： Novel intermediates for the preparation of trienic steroids which intermediates have the formula ##SPC1##Wherein R is alkyl of 1 to 4 carbon atoms and X is selected from the group consisting of aliphatic of 1 to 6 carbon atoms optionally substituted and cycloalkyl of 3 to 6 carbon atoms and Y is selected from the group consisting of =O and ethylenedioxy.
摘要翻译：用于制备三烯类固醇的新型中间体，其中间体具有式WHEREIN R是1至4个碳原子的烷基，X选自具有1-6个碳原子的任选取代的脂肪族和3-6个碳原子的环烷基和 Y选自= O和亚乙二氧基。

8. 发明授权

US3702334A Process for the preparation of 17-substituted-delta4-gonenes and intermediates 失效
标题翻译：制备17-取代的DELTA4-GONENES和中间体的方法
公开(公告)号：US3702334A
公开(公告)日：1972-11-07
申请号：US3702334D
申请日：1970-08-12
申请人： JULIEN WARNANT , JEAN JOLLY , ROBERT JOLY
发明人： WARNANT JULIEN , JOLLY JEAN , JOLY ROBERT
IPC分类号： A41B1/00 , A41B3/00 , C07J1/00 , C07J7/00 , C07J41/00 , C07J73/00 , C07J75/00 , C07C167/02
CPC分类号： C07J73/00 , C07J1/00 , C07J7/00 , C07J41/00 , C07J75/00
摘要： A PROCESS FOR THE PRODUCTION OF A $4-GONENIC STEROID HAVING THE FORMULA

3-(O=),13-R,17-RIV,17-(R''-O-)G0NA-4,9-DIENE

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

9. 发明授权

US4151195A Novel racemization process 失效
标题翻译：新的外消旋化过程
公开(公告)号：US4151195A
公开(公告)日：1979-04-24
申请号：US789843
申请日：1977-04-22
申请人： Julien Warnant , Jacques Prost-Marechal , Philippe Cosquer
发明人： Julien Warnant , Jacques Prost-Marechal , Philippe Cosquer
IPC分类号： A01N53/08 , A01N53/14 , A01P13/00 , C07B31/00 , C07B55/00 , C07C67/00 , C07C69/743 , C07C253/00 , C07C253/30 , C07C255/38 , C07C255/39 , C07C255/53 , C07C121/75
CPC分类号： C07B55/00 , C07C255/53
摘要： A process for the preparation of an ester of chiral (A) acid with a racemic (R,S) .alpha.-cyano-3-phenoxybenzyl alcohol (B) by reacting an ester of chiral (A) acid with .alpha.-cyano-3-phenoxybenzyl alcohol of the formula ##STR1## in its optically active (R) form or (S) form or a mixture of esters of said (R) alcohol and (S) alcohol in non-equimolecular proportions with a base selected from the group consisting of ammonia, primary, secondary and tertiary amines, quaternary ammonium compounds, liquid amines of high molecular weight and a catalytic amount of a strong base in at least one solvent for the starting esters and in which the ester of racemic alcohol is soluble and recovering from the resulting solution the ester of chiral (A) acid with racemic (R,S) alcohol.
摘要翻译：通过使手性（A）酸的酯与α-氰基-3-氰基-3-苯氧基苄醇（B）的制备手性（A）酸的酯与外消旋（R，S）式（I）所示的式（ⅩⅧ）的苯氧基苄醇或其光学活性（R）形式的（S）形式或所述（R）醇和（S）醇的酯与非等分子比例的酯与选自下组的碱由氨，伯，仲和叔胺组成，季铵化合物，高分子量的液态胺和催化量的至少一种用于起始酯的溶剂中的强碱，其中外消旋醇的酯可溶于和回收从所得溶液中将手性（A）酸与外消旋（R，S）醇的酯反应。

10. 发明授权

US3932420A Process for the preparation of glaziovine 失效
标题翻译：制备glaziovine的方法
公开(公告)号：US3932420A
公开(公告)日：1976-01-13
申请号：US444554
申请日：1974-02-21
申请人： Julien Warnant , Andre Farcilli , Italo Medici , Edmond Toromanoff
发明人： Julien Warnant , Andre Farcilli , Italo Medici , Edmond Toromanoff
IPC分类号： C07D217/20 , C07D221/18 , C07D221/20 , C07D217/12
CPC分类号： C07D221/20 , C07D217/20
摘要： Process for the preparation of glaziovine by treating N-methyl bromococlaurine in an inert organic solvent with a tin hydride tri-substituted with organic radicals in the presence of a free radical promoter.
摘要翻译：通过在惰性有机溶剂中用自由基促进剂存在下用有机基团三取代的氢化锡处理N-甲基溴代牛磺酸来制备格列酮的方法。

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