Glycine, N-methyl-, ethyl ester → HCID 86650566、化合物

反応式

Br[C:2]1[CH2:6][CH2:5][O:4][N:3]=1.NC1CCON=1.C([O:15][C:16](=[O:20])[CH2:17][NH:18][CH3:19])C>>[O:4]1[CH2:5][CH2:6][C:2]([N:18]([CH3:19])[CH2:17][C:16]([OH:20])=[O:15])=[N:3]1

参加物

反応物 3

HCID 95849Glycine, N-methyl-, ethyl ester

HCID 122690414,5-Dihydro-1,2-oxazol-3-amine

HCID 219834983-Bromo-4,5-dihydroisoxazole

生成物 1

HCID 86650566HCID 86650566、化合物

実験手順

2-((4,5-dihydroisoxazol-3-yl)(methyl)amino)acetic acid I-244a and I-244b were prepared in 2 steps according to the following procedure: racemic 3-bromo-4,5-dihydroisoxazole I-10 was converted to the corresponding 3-amino-4,5-dihydroisoxazole by reacting it with sarcosine ethyl ester under the same conditions as in Example 238. The ethyl ester was then hydrolyzed using the analogous conditions as in Example 119 to provide a mixture of racemic I-244. These compounds can be separated using chiral HPLC methods known in the art. For example, see chiral HPLC Method disclosed herein. [M−H]−=327.5 m/z. Activity: B