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Фосарбин及其同类物的简易合成法

A SIMPLE SYNTHETIC METHOD OF PHOSARBIN AND ITS HOMOLOGUES (TETRAALKYL MONOTHIOPYROPHOSPHATES)
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摘要 据Ленкевич报道,Фосарбин(一硫代焦磷酸四乙酯)对受600伦照射狗有良好的防治效果。以本制剂~*0.01毫克/公斤于照前或照后给动物皮注,14条狗全部活存,而单照射不给药的对照狗则于照后第11~15天内全死亡。前人把该药的抗放作用归之于胆碱酯酶的抑制作用。近年来曾报道某些胆碱酯酶抑制剂与大力补(蛋白同化激素)伍用可提高抗放效果。而当照射剂量较高时抗放作用更为明显。临床上用本品治疗青光眼,用途较广泛。 A synthetic method for tetraalkylmonothiopyrophosphates has been worked out as follows: Tetraalkylmonothiopyrophosphates (2, R=C_2H_5, i-C_4H_9) were synthesized from the reaction of two moies of the corresponding dialkyl phosphonates with one mole of sulfur in carbon tetrachloride in the presence of excess triethylamine. The yields ranged from 65 to 80%. The method can be modified for the synthesis of unsymmetrical diethyl dialkyl monothiopyrophoshpates (6, R=alkyl=i-C_3H_7, i-C_4H_9, sec-C_4H_9). The reaction mechanism was briefly discussed.
作者 童曾寿
出处 《军事医学》 CAS 1982年第6期715-718,共4页 Military Medical Sciences
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