2-(1-Ethoxycarbonyl-2-vinyl-cyclopropylcarbamoyl)-4-[2-(3,5-difluoro-phenyl)-7-methoxy-8-methyl-quinazolin-4-yloxy]-cyclopentanecarboxylic acid → 1-{[4-[2-(3,5-Difluoro-phenyl)-7-methoxy-8-methyl-quinazolin-4-yloxy]-2-(hex-5-enyl-methyl-carbamoyl)-cyclopentanecarbonyl]-amino}-2-vinyl-cyclopropane-carboxylic acid ethyl ester
Reaction equation
[CH2:1]([O:3][C:4]([C:6]1([NH:11][C:12]([CH:14]2[CH2:18][CH:17]([O:19][C:20]3[C:29]4[C:24](=[C:25]([CH3:32])[C:26]([O:30][CH3:31])=[CH:27][CH:28]=4)[N:23]=[C:22]([C:33]4[CH:38]=[C:37]([F:39])[CH:36]=[C:35]([F:40])[CH:34]=4)[N:21]=3)[CH2:16][CH:15]2[C:41](O)=[O:42])=[O:13])[CH2:8][CH:7]1[CH:9]=[CH2:10])=[O:5])[CH3:2].Cl.[CH2:45]([NH:51][CH3:52])[CH2:46][CH2:47][CH2:48][CH:49]=[CH2:50]>>[CH2:1]([O:3][C:4]([C:6]1([NH:11][C:12]([CH:14]2[CH2:18][CH:17]([O:19][C:20]3[C:29]4[C:24](=[C:25]([CH3:32])[C:26]([O:30][CH3:31])=[CH:27][CH:28]=4)[N:23]=[C:22]([C:33]4[CH:34]=[C:35]([F:40])[CH:36]=[C:37]([F:39])[CH:38]=4)[N:21]=3)[CH2:16][CH:15]2[C:41](=[O:42])[N:51]([CH2:45][CH2:46][CH2:47][CH2:48][CH:49]=[CH2:50])[CH3:52])=[O:13])[CH2:8][CH:7]1[CH:9]=[CH2:10])=[O:5])[CH3:2]Participants
3
Reactant 2
Product 1
Procedure
The acid 167 was reacted with hex-5-enyl-methyl-amine hydrochloride as according to the same procedure described in example 157, which gave the title compound (0.838 g, 81%), LRMS (M+H) 691.
Sources & evidence
- ORD record
- ord-08cb3c2ae77a402986b6eaa5fa49a6fb
- Source dataset
- uspto-grants-2010_02
- Patent number
- US07659245B2
Reaction notes
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