Patent · US Expired

Process for the preparation of an oxirane, aziridine or cyclopropane

US6559323B1 · kind B1 · utility

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Key dates

Filing dateFeb 28, 2000
Grant dateMay 6, 2003
Priority date
Expiry dateFeb 28, 2020

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY10S436/903
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I), wherein X is oxygen, NR4 or CHR5; R1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R2 is hydrogen, alkyl, aryl, heteroaromatic, CO2R8, CHR14NHR13, heterocyclic or cycloalkyl; or R1 and R2 join together to form a cycloalkyl ring; R3 and R10 are, independently, hydrogen, alkyl, aryl, heteroaromatic, CO2R8, R83Sn, CONR8R9, trialkylsilyl or triarylsilyl; R4 is an electron withdrawing group; R5 is alkyl, cycloalkyl, aryl, heteroaromatic, SO2R8, SO3R8, COR8, CO2R8, CONR8R9, PO(R8)2, PO(OR8)2 or CN; R8 and R9 are independently alkyl or aryl; and R13 and R14 are independently hydrogen, alkyl or aryl is provided. The process comprises degrading a compound of formula (II), (IIa), (IIb) or (IIc): wherein R3 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 formula SR6R7, wherein R6 and R7 are independently alkyl, aryl or heteroaromatic, or R6 and R7 join together t…

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.