Process for the preparation of N-[(3-aminooxetan-3-yl) methyl]-2-(1,1-dioxo-3,5-dihydro-1,4-benzothiazepin-4-yl)-6-methyl-quinazolin-4-amine

Patent metadata

Field	Value
Publication number	US-10253022-B2
Application number	US-201815988570-A
Country	US
Kind code	B2
Filing date	May 24, 2018
Priority date	Jan 24, 2014
Publication date	Apr 9, 2019
Grant date	Apr 9, 2019

Abstract

The present invention relates to a novel process for the preparation of a compound of the formula (I):

and pharmaceutically acceptable acid addition salts thereof, which is useful for prophylaxis and treatment of respiratory syncytial virus (RSV) infection in mammal or human being.

First claim

The invention claimed is:

1. A process for the preparation of a compound of the formula (V):

wherein R is C 1-6 alkyl, C 1-6 alkoxyphenyl-C x H 2x — or phenyl-C x H 2x —, and wherein x is 1 to 6,

the process comprising the following steps:
Step a) converting a carboxy group to a carbamate to form a compound of formula (III)

Step b) aminating a compound of formula (III) to form a compound of formula (V)

2. A compound of formula (V):

wherein R is C 1-6 alkyl, C 1-6 alkoxyphenyl-C x H 2x — or phenyl-C x H 2x —, and wherein x is 1 to 6.

3. A compound having the structure:

Assignees

• Hoffmann La Roche

Inventors

• Chen Junli
• Ren Yi
• She Jin
• Wang Lin
• Yu Jianhua
• Zhang Guocai

Classifications

• A61P31/14

  for RNA viruses · CPC title

• C07D417/14 Primary

  containing three or more hetero rings · CPC title

• C07D305/06

  with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms · CPC title

• C07D305/08

  with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring atoms · CPC title

• A61K31/4725

  containing further heterocyclic rings · CPC title