Abstract
In order to obtain effective anti-cancer agents, O-(1-aziridinyl)acetyl-DL-serine, O-(1-aziridinyl)acetyl-N-benzyloxycarbonyl-DL-serine, N-(1-aziridinyl)acetyl-DL-serine, ethyl 1-aziridinylacetate, DL-2-(1-aziridinyl)-3-phenylpropionic acid and its ethyl ester, and DL-2-(1-aziridinyl)succinic acid were synthesized but all showed only a weak action against Ehrlich ascites tumor. During the course of these syntheses, it was found that the use of acetic acid as a solvent in the O-chloro-acetylation of serine with chloroacetyc anhydride only afforded the O-acetyl compound while the use of ethyl acetate or ethyl or methyl chloroacetate as a solvent gave O-chloroacetyl-DL-serine in a good yield.
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