新产品编号:305835

Chemical Name: N-[2-(4-Aminophenyl)-1(S)-[4-(2-fluoroethyl)piperidin-1-ylcarbonyl]ethyl]-4-[1(S)-benzyl-2-(4-morpholinyl)ethyl]pyridine-3-sulfonamide
CAS No. 200270-65-1
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Coupling of N-Boc-p-nitrophenylalanine (I) with 4-(2-fluoroethyl)piperidine (II) by means of 2-benzotriazolyl-1,1,3,3-tetramethyluronium tetrafluoborate (TBTU) gave amide (III) which,after acidic deprotection provided aminoamide (IV).4-Chloropyridine-3-sulfonyl chloride (VI),generated from 4-hydroxy pyridine-3-sulfonic acid (V) by chlorination with PCl5/POCl3,was coupled with amine (IV) to afford sulfonamide (VII).Further condensation of (VII) with L-phenylalaninol (VIII) produced aminopyridine (IX).Conversion of the alcohol group of (IX) to the corresponding mesylate,followed by displacement with morpholine furnished the N-substituted morpholine (X).The nitro group of (X) was finally reduced to the target aniline by hydrogenation over Pd/C.