PKI-75166, PKI-166, CGP-75166

Chemical Name: 4-[4-[1(R)-Phenylethylamino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol
项目整合开发状态: Discontinued
项目研究机构: Novartis (Originator)
合成路线:The cyclization of 4-methoxyphenacyl bromide (I) with 2-amidinoacetic acid ethyl ester (II) by means of sodium ethoxide in ethanol gives 2-amino-5-(4-methoxyphenyl)-1H-pyrrole-3-carboxylic acid ethyl ester (III),which is cyclized with formamide in DMF at 150 C to yield the pyrrolopyrimidine (IV).The reaction of the OH group of (IV) with POCl3 at 150 C affords the corresponding chloro derivative (V),which is condensed with 1(R)-phenylethylamine (VI) in refluxing butanol to provide the adduct (VII).Finally,this compound is demethylated by means of BBr3 in dichloromethane to furnish the target pyrrolopyrimidine.