CAS: 74189-25-6; Benzhydryl 6α-Bromopenicillanate

上下游产品

6-bromopenicillanic acid diazodiphenylmethane diphenylmethyl 6,6-dibromopenicillanate 1,1-Diphenylmethanolbenzhydryl 6,6-dihydropenicillate benzhydryl 6α-(2'-acetoxyethyl)penicillanate benzhydryl 6α-allylpenicillanate benzhydryl 6α-bromopenicillanate S,S-dioxide

📜6-氨基青霉烷酸置于4-二甲氨基吡啶,硫酸,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,Potassium Bromide,Sodium Nitrite体系中,用 二氯甲烷,水 作为反应溶剂,化学反应 0.05H,反应生成 舒巴坦杂质18
参考文献:连续流在他唑巴坦合成中的应用
标题:连续流在他唑巴坦合成中的应用
摘要:他唑巴坦是一种β-内酰胺酶抑制剂.在这项工作中,已经开发了用于合成他唑巴坦的连续流动和间歇实验的组合.前三步和过氧乙酸的制备在微反应器中连续进行,提高了程序的安全性和效率.微反应器中还有脱保护反应的最后一步,可以提高收率,减少杂质的形成.在优化的工艺条件下,目标产品的总收率达到37.09%(批量为30.93%).连续流法不仅大大缩短了反应时间,而且显着提高了程序的安全性,提高了收率.
DOI:10.1021/acs.Oprd.1C00127

专利信息

专利号:US-4283531-A
优先权日:1978-06-02
标 题:Synthesis of β-lactams having a substituted hydroxymethylene group at the position α to the lactam carbonyl group
发明人：GANGULY ASHIT K; GIRIJAVALLABHAN VIYYOOR M; CAVENDER PATRICIA; SARRE OLGA; MCCOMBIE STUART W
权利人:SCHERING CORP
摘要:β-Lactams having a substituted hydroxymethylene group at the position α to the lactam carbonyl group are prepared by reaction of an α-halo-β-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate which in situ reacts with an appropriate aldehyde or ketone. n Also described are novel penicillins and cephalosporins having useful antibacterial activity.