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公开(公告)号：EP0983236A2
公开(公告)日：2000-03-08
申请号：EP98919377.6
申请日：1998-05-01
IPC分类号： C07D203/24 , C07D203/22 , C07D301/02 , C07C13/04
CPC分类号： C07D303/22 , C07D203/02 , C07D301/02 , C07D303/04 , C07D303/08 , C07D303/46 , C07D327/06 , C07D333/54 , C07D333/78 , C07D405/04 , C07D495/08 , Y10S436/903
摘要： A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I) wherein X is oxygen, NR?4 or CHR5; R1¿ is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO¿2?R?8, CHR14NHR13¿, heterocyclic or cycloalkyl; or R?1 and R2¿ join together to form a cycloalkyl ring; R?3 and R10¿ are, independently, hydrogen, alkyl, aryl, heteroaromatic, CO¿2R?8, R83Sn, CONR8R9, trialkylsilyl or triarylsilyl; R4 is an electron withdrawing group; R5 is alkyl, cycloalkyl, aryl, heteroaromatic, SO¿2R?8, SO3R?8, COR8, CO¿2R?8, CONR8R9, PO(R8)¿2, PO(OR8)2 or CN; R?8 and R9¿ are independently alkyl or aryl; and R?13 and R14¿ are independently hydrogen, alkyl or aryl is provided. The process comprises degrading a compound of the formula (II), (IIa), (IIb) or (IIc), wherein R?3 and R10¿ are as defined above; Y is a cation; depending on the nature of Y, r is 1 or 2; and L is a suitable leaving group, to form a diazo compound. The diazo compound is reacted with a suitable transition metal catalyst, and the product thereof reacted with a sulphide of the formula SR6R7, wherein R?6 and R7¿ are independently alkyl, aryl or heteroaromatic, or R?6 and R7¿ join together to form an optionally substituted ring which optionally includes an additional heteroatom. This product is then reacted with an aldehyde, ketone, imine or alkene.
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公开(公告)号：EP0724569B1
公开(公告)日：2003-03-12
申请号：EP94930260.8
申请日：1994-10-19
申请人： Avecia Limited
发明人： AGGARWAL, Varinder, Kumar , ABDEL-RAHMAN, Hesham, Nimer, Hasan , LEE, Hee, Yoon 119-Dong 502-Ho Hanbit Apartment
IPC分类号： C07D203/24 , C07D203/22 , C07D203/02 , C07F9/564 , C07D301/02 , C07D407/04 , C07C13/04 , C07F15/00 , C07F3/06
CPC分类号： C07D203/22 , C07C2/868 , C07C2601/02 , C07D203/02 , C07D203/24 , C07D301/02 , C07D303/04 , C07D303/08 , C07D303/16 , C07D303/40 , C07D303/46 , C07D407/04 , C07F9/564 , C07C13/04
摘要： A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I) wherein, X is oxygen, NR?4 or CHR5; R1¿ is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO¿2?R?8, CHR14NHR13¿, heterocyclic or cycloalkyl; or R?1 and R2¿ join together to form a cycloalkyl ring; R3 is hydrogen, alkyl, aryl, heteroaromatic, CO¿2R?8, R83Sn, CONR8R9 or trimethylsilyl; R?4 and R5¿ are, independently, alkyl, cycloalkyl, aryl, heteroaromatic, SO¿2R?8, SO3R?8, COR8, CO¿2R?8, CONR8R9¿ or CN, or R4 can also be P(O)(aryl)¿2?; R?8 and R9¿ are independently alkyl, aryl or arylalkyl; R?13 and R14¿ are independently hydrogen, alkyl or aryl; the process comprising reacting a mixture of a compound of formula (II), wherein R1, R2 and X are as defined above, and a sulphide of formula SR6R7, wherein R?6 and R7¿ are independently alkyl, aryl or heteroaomatic, or R?6 and R7¿ join together to form a cycloalkyl ring which optionally includes an additional heteroatom, with either (i) a metallocarbon obtainable by reacting an alkylmetal with a methane derivative of formula CHR3X'X'', wherein R3 is as defined above, and X' and X'' are independently, a leaving group, or (ii) a metallocarbon obtainable by reacting a compound of formula (III), (wherein R3 may not be hydrogen) with a suitable organometallic or inorganic reagent.
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公开(公告)号：EP0983236B1
公开(公告)日：2003-09-10
申请号：EP98919377.6
申请日：1998-05-01
IPC分类号： C07D203/24 , C07D203/22 , C07D301/02 , C07C13/04
CPC分类号： C07D303/22 , C07D203/02 , C07D301/02 , C07D303/04 , C07D303/08 , C07D303/46 , C07D327/06 , C07D333/54 , C07D333/78 , C07D405/04 , C07D495/08 , Y10S436/903
摘要： A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I) wherein X is oxygen, NR?4 or CHR5; R1¿ is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO¿2?R?8, CHR14NHR13¿, heterocyclic or cycloalkyl; or R?1 and R2¿ join together to form a cycloalkyl ring; R?3 and R10¿ are, independently, hydrogen, alkyl, aryl, heteroaromatic, CO¿2R?8, R83Sn, CONR8R9, trialkylsilyl or triarylsilyl; R4 is an electron withdrawing group; R5 is alkyl, cycloalkyl, aryl, heteroaromatic, SO¿2R?8, SO3R?8, COR8, CO¿2R?8, CONR8R9, PO(R8)¿2, PO(OR8)2 or CN; R?8 and R9¿ are independently alkyl or aryl; and R?13 and R14¿ are independently hydrogen, alkyl or aryl is provided. The process comprises degrading a compound of the formula (II), (IIa), (IIb) or (IIc), wherein R?3 and R10¿ are as defined above; Y is a cation; depending on the nature of Y, r is 1 or 2; and L is a suitable leaving group, to form a diazo compound. The diazo compound is reacted with a suitable transition metal catalyst, and the product thereof reacted with a sulphide of the formula SR6R7, wherein R?6 and R7¿ are independently alkyl, aryl or heteroaromatic, or R?6 and R7¿ join together to form an optionally substituted ring which optionally includes an additional heteroatom. This product is then reacted with an aldehyde, ketone, imine or alkene.
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