申请人:Research Corporation Technologies, Inc.
公开号:US05101059A1
公开(公告)日:1992-03-31
This invention relates to compounds of the formula a compound of the formula ##STR1## wherein X is O, CR.sub.7 R.sub.8, S or NR.sub.9 wherein R.sub.7 and R.sub.8 are independently hydrogen, or lower alkyl, and R.sub.9 is lower alkyl; n is 0 or 1; R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, monoorganosilyl, diorganosilyl, triorganosilyl, halogen, aryl, or nitro; R.sub.3 is hydrogen, lower alkyl, monoorganosilyl, diorganosilyl, triorganosilyl, halogen, 9-fluorenylalkyl, cycloalkyl, aryl or aralkyl; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or aryl or one of R.sub.4 and R.sub.5 is 9-fluorenyl; R.sub.6 is H or COZ wherein Z is an amino acid, a peptide residue or a leaving group; and with the provisos that when n is 0 and R.sub.3 is hydrogen, R.sub.1 and R.sub.2 are not hydrogen, halogen or nitro; that when n is 0 and R.sub.3 is lower alkyl, R.sub.1 and R.sub.2 are not hydrogen; and that when X is O or CR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are H, that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are not all simultaneously H. The compounds of the present invention are useful in peptide synthesis as blocking or protecting groups for reactive groups. The present invention is also directed to a method of protecting a reactive group of an organic molecule during a reaction which modifies a portion of the molecule other than the protected group.
本发明涉及公式化合物,该化合物的公式为##STR1##其中X为O,CR.sub.7 R.sub.8,S或NR.sub.9,其中R.sub.7和R.sub.8独立地为氢或低碳基,R.sub.9为低碳基;n为0或1;R.sub.1和R.sub.2独立地为氢,低碳基,单基硅烷基,双基硅烷基,三基硅烷基,卤素,芳基或硝基;R.sub.3为氢,低碳基,单基硅烷基,双基硅烷基,三基硅烷基,卤素,9-芴基烷基,环烷基,芳基或芳基烷基;R.sub.4和R.sub.5独立地为氢,低碳基或芳基,或R.sub.4和R.sub.5中的一个为9-芴基;R.sub.6为H或COZ,其中Z为氨基酸,肽残基或离去基;并且当n为0且R.sub.3为氢时,R.sub.1和R.sub.2不是氢,卤素或硝基;当n为0且R.sub.3为低碳基时,R.sub.1和R.sub.2不是氢;当X为O或CR.sub.7R.sub.8,其中R.sub.7和R.sub.8为H时,R.sub.1、R.sub.2、R.sub.3、R.sub.4、R.sub.5和R.sub.6不同时为H。本发明的化合物可用于肽合成中,作为反应基团的阻断或保护基团。本发明还涉及一种在反应过程中保护有机分子的反应基团的方法,该反应修改分子的除保护基团以外的部分。