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1.发明授权Trialkylsilyl trifluoromethanesulfonate mediated .alpha.-methylenic carbon functionalization of 4-aza-5.alpha.-androstan-3-one steroids 失效三氮代三氟甲磺酸三烷基甲硅烷基酯介导的4-氮杂-5α-雄甾烷-3-酮类固醇的α-亚甲基碳官能化
公开(公告)号：US5187278A
公开(公告)日：1993-02-16
申请号：US786615
申请日：1991-11-01
申请人： Anthony O. King , Kevin Anderson , Sandor Karady , Alan W. Douglas , Newton L. Abramson , Richard F. Shuman
发明人： Anthony O. King , Kevin Anderson , Sandor Karady , Alan W. Douglas , Newton L. Abramson , Richard F. Shuman
IPC分类号： C07J73/00
CPC分类号： C07J73/005
摘要： A novel single-pot trialkylsilyl trifluoromethanesulfonate (R.sub.3 Si-OTf) mediated process produces derivatives of 4-aza 3-keto steroids at the .alpha.-methylenic carbon through electrophilic substitution. These derivatives are useful in the preparation, through elimination of the substituent on the .alpha.-methylene carbon, of .DELTA.-1 olefin 4-aza 3-keto steroids which are potent inhibitors of 5-.alpha. reductase.
摘要翻译： 一种新的单罐三烷基甲硅烷基三氟甲磺酸盐（R3Si-OTf）介导的方法通过亲电取代产生α-甲基碳上的4-氮杂-3-酮类固醇衍生物。 这些衍生物可用于通过消除α-亚甲基碳上的取代基的DELTA-1烯烃4-氮杂-3-酮类固醇，其是5-α还原酶的有效抑制剂。
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2.发明授权Process for iodinating or brominating the .alpha.-methylenic carbon of a secondary amide 失效二次酰胺（ALPHA） - 甲基二氧化碳的改性或改性方法
公开(公告)号：US5120847A
公开(公告)日：1992-06-09
申请号：US572920
申请日：1990-08-27
IPC分类号： A61K31/395 , C07C231/12 , C07C233/04 , C07D223/10 , C07D223/16 , C07D233/04 , C07D233/10 , C07D233/16 , C07J51/00 , C07J73/00 , C07J75/00
CPC分类号： C07D223/16 , C07C231/12 , C07D223/10 , C07J73/005
摘要： A novel, facile, and specific process for .alpha.-iodinating or .alpha.-brominating the .alpha.-methylenic carbon of a straight chain, branched chain, or cyclic secondary amide, such as a lactam or an azasteroid, comprises reacting the amide with trialkylsilyl-X (R.sub.3 Si--X), where X is Br, I, or Cl, and R is methyl, ethyl, or n-propyl, in the presence of I.sub.2 or Br.sub.2. The .alpha.-iodo- or .alpha.-bromo-amide is useful for making the .alpha.,.beta.-unsaturated amide through dehydrohalogenation.
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3.发明授权Ortho-lithiation process for the synthesis of 2-substituted 1-(tetrazol-5-yl)benzenes 失效用于合成2-取代的1-（四唑-5-基）苯的正电子锂化方法
公开(公告)号：US5039814A
公开(公告)日：1991-08-13
申请号：US517889
申请日：1990-05-02
IPC分类号： A61K31/41 , A61P43/00 , C07D257/04
CPC分类号： C07D257/04
摘要： A process utilizes the tetrazole functional group to direct lithiation at the ortho position of a phenyltetrazole and generate a nucleophilic aryllithium species which then undergoes reaction with an electrophile to generate a 2-substituted 1-(tetrazol-5-yl)benzene. The process is useful in the production of intermediates in the synthesis of angiotensin II antagonists. This novel process is a more cost effective and versatile route for the large-scale preparation of these key intermediates.
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公开(公告)号：US4942235A
公开(公告)日：1990-07-17
申请号：US324138
申请日：1989-03-16
IPC分类号： C07D471/20 , C07D491/22 , C07D495/22
CPC分类号： C07D471/20 , C07D491/22 , C07D495/22
摘要： A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizine-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2-yl)amino]ethyl]methanesulfonamide is described.
摘要翻译： 特别是（2R-反式）-N- [2-（1,3,4,6,7,12b-六氢-2'-氧代螺[aro- [2']）的制备某些（2R-反式）六氢喹诺酮， （2R-反式）-N- [2 - [（2-氰基 - （1,3,4,5-四氢 - 咪唑并[3,2-a]喹喔啉-2,3'-基] -3'-基）乙基） - 甲磺酰胺 6,7,12b-六氢 - 氨基 - [2,3-a]喹啉-2-基）氨基]乙基]甲磺酰胺。
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5.发明授权Process for selective mono-debromination of polybromoalkyl aryl or heteroaryl ketones 失效聚溴烷基芳基或杂芳基酮的选择性单脱溴方法公开(公告)号：US06271421B1
公开(公告)日：2001-08-07
申请号：US09439821
申请日：1999-11-12
申请人： Anthony O. King
发明人： Anthony O. King
IPC分类号： C07C4565
CPC分类号： C07C45/65 , C07C45/63 , C07D307/80
摘要： A process for selectively debrominating polybromoalkyl aryl ketones and polybromoalkyl heteroaryl ketones is disclosed. The process comprises contacting an alpha-polybrominated ketone with an alkali metal sulfite in the presence of a C2-C6 alkylcarboxylic acid to obtain a selectively mono-debrominated product.
摘要翻译： 公开了一种选择性脱溴多溴烷基芳基酮和多溴烷基杂芳基酮的方法。 该方法包括在C 2 -C 6烷基羧酸的存在下使α-多溴代酮与碱金属亚硫酸盐接触以获得选择性单脱溴产物。
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6.发明授权Process for the preparation cis-(1S,2R)-indanediol by direduction of 1,2-indanedione using trichosporon cutaneum 失效通过使用trichosporon cutaneum引导1,2-茚满酮制备顺式 - （1S，2R） - 茚满二醇的方法公开(公告)号：US06171832B2
公开(公告)日：2001-01-09
申请号：US09300344
申请日：1999-04-27
IPC分类号： C12P722
CPC分类号： C12P7/18 , Y10S435/911
摘要： A process for preparing cis-(1S,2R)-indanediol is disclosed. The process comprises (A) fermenting a culture medium containing a yeast strain selected from the group consisting of Trichosporon cutaneum MY 1506 (ATCC 74440) and mutants thereof and 1,2-indanedione to form cis-(1S,2R)-indanediol; and (B) recovering cis-(1S,2R)-indanediol from the culture medium. A process for preparing (1S)-amino-(2R)-indanol from the recovered cis-(1S,2R)-indanediol via the Ritter reaction is also disclosed.
摘要翻译： 公开了制备顺式 - （1S，2R） - 1,2-二醇的方法。 该方法包括（A）发酵含有选自Trichosporon cutaneum MY 1506（ATCC 74440）及其突变体和1,2-茚二酮的酵母菌株以形成顺式 - （1S，2R） - 茚满二醇的培养基; 和（B）从培养基中回收顺式 - （1S，2R） - 1,2-二醇。 还公开了通过Ritter反应从回收的顺式 - （1S，2R） - 1,2-二醇制备（1S） - 氨基 - （2R） - 茚满的方法。
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7.发明授权Processes and intermediates for the preparation of 5-oxygenated HMG-CoA reductase inhibitors 失效制备5-氧化型HMG-COA还原酶抑制剂的方法和中间体
公开(公告)号：US5059696A
公开(公告)日：1991-10-22
申请号：US493595
申请日：1990-03-15
申请人： Robert K. Anderson , Ann E. DeCamp , Alan T. Kawaguchi , Anthony O. King , Sander G. Mills , Ralph P. Volante
发明人： Robert K. Anderson , Ann E. DeCamp , Alan T. Kawaguchi , Anthony O. King , Sander G. Mills , Ralph P. Volante
IPC分类号： A61K31/35 , A61K31/351 , A61P3/06 , C07D309/30 , C07F7/18
CPC分类号： C07D309/30 , C07F7/1856
摘要： This invention discloses novel intermediates and novel process for their preparation where said intermediates are useful for the preparation of 5-oxygenated derivatives (T) of lovastatin and analogs thereof at the 8-acyl side chain and 6-position of the polyhydronaphthyl ring. Said derivatives of lovastatin (T) and analogs thereof are useful in treating hypercholesterolemia and are disclosed in the U.S. Pat. No. 4,963,538. ##STR1##
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公开(公告)号：US5545758A
公开(公告)日：1996-08-13
申请号：US289077
申请日：1994-08-11
IPC分类号： C07B41/02 , C07B41/06 , C07B53/00 , C07D215/14 , C07D215/18 , C07D417/06 , C07D495/04 , C07F5/02
CPC分类号： C07D495/04 , C07D215/14 , C07D215/18 , C07F5/027 , Y02P20/55
摘要： The present invention relates to an improved process for the in situ preparation of diisopinocampheylchloroborane which comprises reacting sodium borohydride and boron trichloride with .alpha.-pinene. The diisopinocampheylchloroborane thus obtained may be used, without isolation, to reduce prochiral ketones to their corresponding alcohols in high optical purity.
摘要翻译： 本发明涉及一种二异蒎烷基氯代硼烷的原位制备改进方法，其包括使硼氢化钠和三氯化硼与α-蒎烯反应。 这样得到的二蒎烯yl yl chlor chlor ob or or may。。。。。。。，，，。。。。。。。。。。。。。
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公开(公告)号：US5089626A
公开(公告)日：1992-02-18
申请号：US571398
申请日：1990-08-23
申请人： Anthony O. King
发明人： Anthony O. King
IPC分类号： C07D403/10
CPC分类号： C07D403/10
摘要： There is disclosed a process for preparing the active metabolite of an angiotensin II antagonist from its pro-drug compound.
摘要翻译： 公开了从其原药化合物制备血管紧张素II拮抗剂的活性代谢物的方法。
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公开(公告)号：US5064964A
公开(公告)日：1991-11-12
申请号：US506056
申请日：1990-04-09
IPC分类号： C07D471/20 , C07D491/147 , C07D491/22 , C07D495/22
CPC分类号： C07D471/20 , C07D491/22 , C07D495/22
摘要： A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizine-2,4'-imidazolidin]-3'-yl) ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2-yl)amino]ethyl]methanesulfonamide is described.
摘要翻译： 特别是（2R-反式）-N- [2-（1,3,4,6,7,12b-六氢-2'-氧代螺[aro- [2']）的制备某些（2R-反式）六氢喹诺酮， （2R-反式）-N- [2 - [（2-氰基 - （1,3,4,5-四氢 - 咪唑并[3,2-a]喹喔啉-2,3'-基] -3'-基）乙基） - 甲磺酰胺 6,7,12b-六氢 - 氨基 - [2,3-a]喹啉-2-基）氨基]乙基]甲磺酰胺。
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