CL-329167

4(3H)-喽喴唑酮,2-丁基-6-(1-甲氧基-1-甲基乙基)-3-[[2'-(2H-四唑-5-基)[1,1'-双苯基]-4-基]甲基]-Chemical Name: 2-Butyl-6-(1-methoxy-1-methylethyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]quinazolin-4(3H)-one
CAS No. 143945-39-5, 144364-95-4 (Na salt)
项目整合开发状态: Phase II
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:The cyclization of 2-amino-5-iodobenzoic acid (I) with pentanoic anhydride (II) in basic medium gives 2-butyl-6-iodoquinazolin-4(3H)-one (III),which is condensed with CO and methanol by means of PdCl2(PPh3)2 and TEA yielding 2-butyl-4-oxo-3,4-dihydroquinazoline-6-carboxylic acid methyl ester (IV).The Grignard condensation of (IV) with methylmagnesium bromide affords the tertiary alcohol (V),which is finally condensed with the tetrazolylbiphenyl (VI) by means of LiOMe,methylated at the tertiary alcohol with methyl iodide and NaH,and deprotected with NaOH in methanol/THF.