Semi-synthetic lipopeptides, compositions containing said lipopeptides,
申请人:Merck & Co., Inc.
公开号:US05516757A1
公开(公告)日:1996-05-14
There are disclosed novel semi-synthetic lipopeptides of the formula (Seq. ID Nos. 1-6) ##STR1## wherein the substituents are defined herein, which show utility as antifungal and anti-Pneumocystis agents. Pharmaceutical compositions containing said compounds are also disclosed.
本发明揭示了公式(Seq. ID Nos. 1-6)的新型半合成脂肽##STR1##,其中所述取代基在此处定义,具有作为抗真菌和抗肺孢子虫药物的用途。还公开了含有该化合物的药物组合物。
Alkyl- und Arylsulfens�ureamide durch Cycloeliminierung von Alkenen aus Sulfimiden, 3: Bildung prim�rer und sekund�rer aliphatischer Sulfenamide des TypsRSNH2 bzw.RSNHR 1
作者:Walter Franek、Peter K. Claus
DOI:10.1007/bf00810863
日期:——
Ross,B. et al., Chemische Berichte, 1971, vol. 104, p. 2241 - 2245
作者:Ross,B. et al.
DOI:——
日期:——
Gas-phase SN2 and E2 reactions of alkyl halides
作者:Charles H. DePuy、Scott Gronert、Amy Mullin、Veronica M. Bierbaum
DOI:10.1021/ja00180a003
日期:1990.11
nucleophile and for methyl bromide with HS − as the nucleophile; in both cases the overall reaction exothermicity is about 30 kcal mol −1 . Earlier conclusions that these halides react slowly with stronger bases are shown to be in error. In the region where the rates are slow oxygen anions react with the alkyl chlorides and bromides by elimination while sulfur anions of the same basicity react by substitution
已测量甲基、乙基、正丙基、异丙基、叔丁基和新戊基氯化物和溴化物与以下亲核试剂的气相反应的速率系数,按碱度递减的顺序列出:HO - 、CH 3 O - 、F - 、HO - (H 2 O)、CF 3 CH 2 O - 、H 2 NS - 、C 2 F 5 CH 2 O - 、HS - 和Cl - 。对于氯甲烷,反应效率首先显着低于 1,以 HO - (H 2 O) 作为亲核试剂,而对于甲基溴,以 HS - 作为亲核试剂;在这两种情况下,总反应放热度约为 30 kcal mol -1 。这些卤化物与强碱反应缓慢的早期结论被证明是错误的。在速率较慢的区域,氧阴离子通过消除与烷基氯化物和溴化物反应,而相同碱度的硫阴离子通过取代反应。这种差异是由于硫碱的消除速度减慢;与相同碱度的氧阴离子相比,硫阴离子没有增加亲核性
FRANEK, WALTER;CLAUS, PETER K., MONATSH. CHEM., 121,(1990) N-7, C. 539-547