D-(-)-α-磺苄西林钠的合成工艺改进

Improved synthesis of optical active D-(-)-α-sulbenicillin disodium

目的改进D-(-)-α-磺苄西林钠的合成工艺。方法以苯乙酸为起始原料,经磺化、碱化、离子交换后得消旋的磺苯乙酸,制得磺苯乙酰氯后,与6-APA缩合得到磺苄西林的非对映异构体。通过重结晶的方法分离出D-(-)-α-磺苄西林,再与异辛酸钠成盐制得目标化合物。结果及结论成功地制备了D-(-)-α-磺苄西林钠,缩短了合成路线并节约了成本,更利于工业化生产。

OBJECTIVE To modify the process to synthesize optical active D-（-）-α-sulbenicillin disodium.METHODS The racemic α-sulfophenylacetate was obtained by sulfonation,alkalization and ion exchange of the starting material phenylacetic acid.After the compound was transferred to α-sulfophenylacetyl chloride,the racemic sulbenicillin was produced by condenscition with 6-APA.By the means of recrystallization,the optical active D-（-）-α-sulbenicillin was separated.Finally,the targeting compound D-（-）-α-sulbenicillin disodium was obtained following treatment by sodium iso-octoate.RESULTS and CONCLUSION The targeting compound D-（-）-α-sulbenicillin disodium was successfully synthesized.This synthesis progress is simple,low-cost and easy for industrial production.