反应 #91962

反应方程式

2-bromo-4-fluorobenzaldehyde

thiazole-2-carboxamidine

ethyl acetoacetate

(S)-morpholine-3-carboxylic acid

methyl acetoacetate

(S)-4,4-difluoro-pyrrolidine-2-carboxylic acid

5-methyl-oxazole-4-carboxamidine

→

title compound

(S)-4-[(R)-6-(2-Bromo-4-fluoro-phenyl)-5-ethoxycarbonyl-2-(5-methyl-oxazol-4-yl)-3,6-dihydro-pyrimidin-4-ylmethyl]-morpholine-3-carboxylic acid

反应条件

实验过程

The title compound was prepared in analogy to Example 1 with Procedure A shown in Scheme 4 by using 2-bromo-4-fluorobenzaldehyde, 5-methyl-oxazole-4-carboxamidine (Compound AB), ethyl acetoacetate and (S)-morpholine-3-carboxylic acid instead of 2-chloro-4-fluorobenzaldehyde, thiazole-2-carboxamidine, methyl acetoacetate and (S)-4,4-difluoro-pyrrolidine-2-carboxylic acid. The stereochemistry of Example 69 was determined by comparing its 1H NMR data and HPLC retention time with Example 2.

来源