Sarizotan, EMR-62225, EMD-128130

(-)-(R)-N-(3,4-二氢-2H-1-苯并呋喃-2-基甲基)-N-[5-(4-氟苯基)-3-吡啶甲基]胺Chemical Name: (-)-(R)-N-(3,4-Dihydro-2H-1-benzofuran-2-ylmethyl)-N-[5-(4-fluorophenyl)-3-pyridylmethyl]amine
CAS No. 177975-08-5
项目整合开发状态: Phase III
项目研究机构: Merck KGaA (Originator)
合成路线:Addition of KCN to 3-(2-hydroxyphenyl)propanal (I) produced 2-cyanochromane (II),which was further reduced to the aminomethyl chromane rac-(III) by catalytic hydrogenation.Resolution of this racemic amine by recrystallization of the diastereomeric salts with N-tosyl-L-proline furnished the required (R)-enantiomer (III).Alkylation of amine (III) with 3-(chloromethyl)-5-(4-fluorophenyl)pyridine (IV) in the presence of N-methylmorpholine yielded the target secondary amine.