| abstract |
The present invention relates to (i) alkyl metal methane derivatives of the formula CHR 3 X′X ″ wherein R 3 is hydrogen, alkyl, aryl, heteroaromatic, CO 2 R 8 , R 8 3 Sn, CONR 8 R 9 or trimethylsilyl X ′ and X ″ are each independently a leaving group), or (ii) reacting a compound of formula (III) with a suitable organometallic or inorganic reagent And metal sulfides of the following formula (II) compounds and the formula SR 6 R 7 (wherein R 6 and R 7 are each independently alkyl, aryl or heteroaromatic, or R 6 and R 7 And reacting the mixture optionally to form a cycloalkyl ring comprising additional heteroatoms). The process relates to the preparation of the oxirane, aziridine or cyclopropane of formula (I).n n n n n n n n Wherein X is oxygen, NR 4 or CHR 5 ; R 1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R 2 is hydrogen, alkyl, aryl, heteroaromatic, CO 2 R 8 , CHR 14 NHR 13 , heterocyclic or cycloalkyl; Or R 1 and R 2 join together to form a cycloalkyl ring; R is hydrogen, alkyl, and heteroaromatic, CO 2 R 8 , R 8 3 Sn, CONR 8 R 9 or trimethylsilyl; R 4 and R 5 are each independently alkyl, cycloalkyl, aryl, heteroaromatic, SO 2 R 8 , SO 3 R 8 , COR 8 , CONR 8 R 9 or CN, or R 4 is also P (O) (Aryl) can be 2 ; R 8 and R 9 are each independently alkyl, aryl or arylalkyl; R 13 and R 14 are each independently hydrogen, alkyl or aryl.n n n n n n n n [Wherein R 1 , R 2 and X are as defined above.n n n n n n n n [Wherein R 3 is not hydrogen. |