摘要
4-乙基-2,3-二氧代哌嗪经三光气氯代、与D-苏氨酸缩合、甲酸氧化及草酰氯酰氯化制得2-[(4-乙基-2,3-二氧代-1-哌嗪基)甲酰胺基]-3-甲酰氧基丁酰氯(6),6再与7β-氨基-7α-甲氧基-3-(1-甲基-1H-四唑-5-基硫甲基)-8-氧代-5-硫-1-氮杂二环[4.2.0]辛-2-烯-2-甲酸二苯甲酯(7-MAC)经缩合、脱二苯甲基保护基和脱甲酰基等反应得到抗菌剂头孢拉宗,总收率约5%。
Cefbuperazone was synthesized from 4-ethyl-2,3-dioxopiperazine by chlorination with triphosgene,condensation with D-threonine,oxidation with formic acid and chlorination with oxalyl chloride to give 2-[（4-ethyl-2,3-dioxopiperazin-1-carbonyl）amino]-3-formyloxybutyryl chloride,which was subjected to condensation with diphenylmethyl 7β-amine-7α-methoxy-3-[（1-methyl-1H-tetrazol-5-ylthio）methyl]-8-oxo-5-thio-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate（7-MAC） followed by deprotection of diphenylmethyl group and formyl group. The total yield was about 5%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2010年第9期649-651,共3页
Chinese Journal of Pharmaceuticals
关键词
头孢拉宗
抗菌剂
合成
cefbuperazone
antibacterial agent
synthesis
