US 2019/0100527 A1 · Process For Preparing AD-35

Abstract

Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.

Claims19

Dependent claims

A compound of Formula V:

A method for preparing a compound represented by Formula (I),

comprising the following steps:
(a) coupling a spirocyclopropane lactam shown by Formula V with a compound shown by Formula VI under the action of a base to obtain a compound shown by the Formula VII:
wherein R1 is a protecting group of amino, preferably tert-butoxycarbonyl (Boc);
R2 is halogen or p-toluenesulfonyloxy;
(b) removing a protecting group of amino of the compound shown by Formula VII to obtain a compound shown by Formula VIII or a salt thereof:
wherein R1 is an protecting group of amino, preferably tert-butyloxycarbonyl (Boc);
(c) reacting the compound shown by Formula VIII or a salt thereof with a compound shown by Formula IX or a salt thereof under the action of a base to obtain a compound shown by Formula XI:
wherein Y is halogen or sulfonyloxy;
(d) reacting the compound shown by Formula XI with phosphoric acid to obtain the compound of Formula I:

6 more elements

Dependencies are inferred from the claim text.

Process For Preparing AD-35

Life of this patent

Process For Preparing AD-35

Life of this patent

Abstract

Claims19