96-30-0

2-Chloro-N-methylacetamide is an intermediate used to prepare piperidinylamino pyrrolopyrimidines as selective Janus kinase inhibitors for the treatment of autoimmune diseases and organ transplant rejection.

To methylamine hydrochloride (896 mg, 13.3 mmol) and Na2C03 (5630 mg, 53 mmol) in water (26 mL) was added 2-chloroacetyl chloride (1500 mg, 13.3 mmol). The mixture was stirred at r.t. for lh and extracted with EtOAc (2x). The combined organic layers were dried over Na2S04 and concentrated to provide 2-Chloro-N-methylacetamide (1200 mg, 84%).

[1] Journal of the Chemical Society. Perkin Transactions 2, 2000, # 9, p. 1819 - 1831
[2] Patent: WO2016/210330, 2016, A1. Location in patent: Paragraph 0180-0181
[3] Journal of the Chemical Society. Perkin Transactions 1, 2001, # 1, p. 87 - 93