Synthesis of N ‐[4‐[2‐(2,4‐Diamino‐1,6‐dihydro‐6‐oxo‐5‐pyrimidinyl)‐ethylamino]benzoyl]‐L‐glutamic acid. An acyclic analogue of 5,6,7,8‐tetrahydrofolic acid

The synthesis of N ‐[4‐[2‐(2,4‐diamino‐1,6‐dihydro‐6‐oxo‐5‐pyrimidinyl)ethylamino]benzoyl]‐L‐glutamic acid ( 2 ), a two carbon analogue of 5‐DACTHF ( 1 ) and an acyclic analogue of 5,6,7,8‐tetrahydrofolic acid, is reported. The pyrimidinylacetaldehyde diethyl acetal 3 , which was prepared in 2‐steps from 2‐chloro acetaldehyde diethyl acetal, was converted to 2 in four steps. Compound 2 was less cytotoxic toward Detroit 98 or L cells than 5‐DACTHF ( 1 ).