反应 #67640

ord-33e117da437743818d6eadef14513599

反应方程式

CC(=O)Nc1nc2c(s1)CNCC2
Compound 1035
CC(=O)Nc1nc2c(s1)CNCC2
N-(4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide
Clc1cnccn1
2-chloro pyrazine
O
water
CC(=O)Nc1nc2c(s1)CN(c1cnccn1)CC2
N-(5-(pyrazin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide
收率 9.7%

溶剂

反应条件

温度
250°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    过滤the crude product collected by filtration
  2. 2
    其他The crude solid was purified by silica gel chromatography (CH2Cl2 to EtOH)

实验过程

As shown in step 10-iv of Scheme 10, to a solution of 50 mg of Compound 1035 in 3 mL of NMP was added 100 mg of 2-chloro pyrazine. The reaction mixture was warmed to 250° C. for 10 minutes under microwave irradiation. The reaction was poured into water (10 mL) and the crude product collected by filtration. The crude solid was purified by silica gel chromatography (CH2Cl2 to EtOH) to provide N-(5-(pyrazin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide (Compound 1, 6.8 mg): ESMS (M+H) 276.16.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08524906B2uspto-grants-2013_09