Rationally designed" dipeptoid" analogs of CCK.. alpha.-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent …

…, JC Hunter, MC Pritchard, RS Richardson…

Index: Horwell, David C.; Hughes, John; Hunter, John C.; Pritchard, Martyn C.; Richardson, Reginald S.; at al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 404 - 414

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Citation Number: 195

Abstract

(RS)-2-amino-l-phenylethanol or (5')-phenylalaninol, respectively [DCC, HOBt (PFP), EtOAc]. Acylation of the free hydroxyl groups (succinic anhydride, DMAP, EtOAc) yielded the corresponding hydrogen succinate half-esters 12 and 14 in good yield (Scheme 11). Representative a-substituted phenethylamides were prepared from intermediate 16 (Scheme 111). Coupling 1Oc to 6a (DCC, PFP, EtOAc) gave azide 15, which was ...