| 摘要 |
<p>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.</p> |
