CAS: 58653-97-7; Methyl 2-Methyloxirane-2-Carboxylate

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111058-32-3 4538-50-5 86884-90-4

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CAS号80-62-6 甲基丙烯酸甲酯 | CAS号96-66-2 4,4'-硫联二(6-叔丁基-... | CAS号186581-53-3 重氮甲烷 | CAS号600-22-6 丙酮酸甲酯 | CAS号339530-91-5 3-(4-氟苯巯基)-2-羟基... | CAS号4587-00-2 2-乙酰基-2-甲基环氧乙烷

📜甲基丙烯酸甲酯置于间氯过氧苯甲酸体系中,用 环己烷 作为反应溶剂,以49%的收率获得产物2-甲基缩水甘油酸甲酯
参考文献:2,2-二取代环氧化物的区域选择性羰基化:酮基羟醛产品的替代途径
标题:2,2-二取代环氧化物的区域选择性羰基化:酮基羟醛产品的替代途径
摘要:我们报告了 2,2-二取代环氧化物到 β,β-二取代 β-内酯的区域选择性羰基化.机理研究表明,环氧化物开环是周转限制步骤,这一见解有助于使用弱供体的醚溶剂开发改进的反应条件.广泛的环氧化物可以羰基化为 β-内酯,随后开环产生基于酮的醛醇加合物,为 Mukaiyama 醛醇反应提供替代方案.对映纯的环氧化物被证明经过羰基化/开环过程并保留立体化学以形成对映纯的 β-羟基酯.
DOI:10.1021/jacs.8B12286

专利信息

专利号:US-7199257-B1
优先权日:1999-06-10
标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide
发明人：SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS
权利人:RICHTER GEDEON VEGYESZET
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.

专利号:EP-1614677-B1
优先权日:2004-06-17
标 题 :Improved procedure for the synthesis of bicalutamide
发明人：PIZZATTI ENRICA; VIGANO' ENRICO; LUSSANA MASSIMILIANO; LANDONIO ERNESTO
权利人:COSMA S P A
摘要:The object of the invention is an improved procedure for the synthesis of bicalutamide, characterised in that the 2-hydroxy-2-methyl-3-(4-fluorophenylthio) propionic acid initially produced undergoes a step to acylate the hydroxyl group in position 2 to give an intermediate 2-acyloxy-2-methyl-3-(4-fluorophenylthio) propionic acid, which allows the formation of a successive N-[4-cyano-3-(trifluoromethyl)-phenyl-]-3-[4-fluorophenylthio]-2-acyloxy-2-methyl-propionamide intermediate.

专利号:US-6593492-B1
优先权日:1999-10-27
标 题 :Resolution of intermediates in the synthesis of substantially pure bicalutamide
发明人：EKWURIBE NNOCHIRI NKEM; JAMES KENNETH D
权利人:NOBEX CORP
摘要:A methods of preparing a substantially pure enantiomer of an acylanilide such as Casodex(R) (bicalutamide) and/or its derivatives includes resolving an intermediate compound having the structure of Formula I:whereinR1 is alkyl or haloalkyl having up to 4 carbons;R2 is alkyl having up to 6 carbon atoms;R3 is a direct link or alkyl having up to 6 carbon atoms;R4 is alkyl, alkenyl, hydroxyalkyl or cycloalkyl each of up to 6 carbons; or R4 is phenyl which bears one, two or three substituents independently selected from hydrogen, halogen, nitro, carboxy, carbamoyl and cyano, and alkyl, alkoxy, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, perfluoroalkyl, perfluoroalkylthio, perfluoroalkylsulphinyl, perfluoroalkylsulphonyl, alkoxycarbonyl and N-alkylcarbamoyl each of up to 4 carbon atoms, and phenyl, phenylthio, phenylsulphinyl and phenylsulphonyl; or R4 is naphthyl; or R4 is a 5- or 6-membered saturated or unsaturated heterocyclic which contains one, two or three heteroatoms selected from oxygen, nitrogen and sulfur, which heterocyclic may be a single ring or may be fused to a benzo-ring, and which heterocyclic is unsubstituted or bears one or two halogen, cyano or amino, or alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl each of up to 4 carbon atoms, or oxy or hydroxy substituents, or which if sufficiently saturated may bear one or two oxo substituents; andX1 is oxygen, sulfur, sulphinyl (-SO-), sulphonyl (-SO2-), imino (-NH-) or alkylimino (-NR5-) where R5 is alkyl having up to 6 carbon atoms.The resolved intermediate compound of Formula I is then treated under conditions sufficient to provide a substantially pure enantiomer of an acylanilide such as Casodex(R) (bicalutamide) and/or its derivatives.

专利号:EP-1614677-A2
优先权日:2004-06-17
标 题:Improved procedure for the synthesis of bicalutamide

专利号:US-2005059632-A1
优先权日:2003-06-30
标题 :Synthesis of beta-L-2'-deoxy nucleosides

专利号:WO-2005003374-A2
优先权日:2003-06-30
标题 :SYNTHESIS OF β-L-2-DEOXY NUCLEOSIDES