abstract |
This invention relates to a process for the preparation of an α-chloroketonencompound comprising the steps ofn (i) cyclizing an alkynyl amide to form a 5-methyleneoxazolinen (ii) chlorinating the 5-methyleneoxazoline using trichloroisocyanuric acidnto produce a chlorinated oxazoline intermediaten nand (iii) hydrolyzing the chlorinated oxazoline intermediate with an aqueousnacid to produce the desired monochloroketonen nwhereinn Z is alkyl or substituted alkyl, aryl or substituted aryl, heteroaryl ornsubstituted heteroaryl or phenylene, R is a hydrogen atom or alkyl, and R 1 and R 2 are each independently an alkyl or substituted alkyl group, or R 1 nand R 2 together with the carbon atom to which they are attached form a cyclicnstructure. n Additionally, when R is a hydrogen atom, a dichloroketone can benconveniently formed through adjustment of reaction conditions. |