5-Amino-2-(trifluoromethyl)pyridine → HCID 58700383、化合物

反応式

C(OC(N1CCC2N(C)C3C(C(F)(F)F)=CC(NC4C=CC=CN=4)=CC=3C2C1)=O)(C)(C)C.C(OC([N:40]1[CH2:56][CH2:55][C@@H:43]2[N:44]([CH3:54])[C:45]3[C:46]([C:52]#[N:53])=[CH:47][C:48](Br)=[CH:49][C:50]=3[C@@H:42]2[CH2:41]1)=O)(C)(C)C.[F:57][C:58]([F:67])([F:66])[C:59]1[N:64]=[CH:63][C:62]([NH2:65])=[CH:61][CH:60]=1.CC([O-])(C)C.[Na+]>>[CH3:54][N:44]1[C:45]2[C:50](=[CH:49][C:48]([NH:65][C:62]3[CH:63]=[N:64][C:59]([C:58]([F:67])([F:57])[F:66])=[CH:60][CH:61]=3)=[CH:47][C:46]=2[C:52]#[N:53])[C@@H:42]2[CH2:41][NH:40][CH2:56][CH2:55][C@H:43]12

参加物

反応物 4

HCID 27377445-Amino-2-(trifluoromethyl)pyridine

HCID 23676156Sodium t-butoxide

HCID 58700289(4aS,9bR)-8-bromo-6-cyano-5-methyl-1,3,4,4a,5,9b-hexahydro-pyrido[4,3-b]indole-2-carboxylic acid tert-butyl ester

HCID 671835315-Methyl-8-(pyridinylamino)-6-trifluoromethyl-1,3,4,4a,5,9b-hexahydro-pyrido[4,3-b]indole-2-carboxylic acid tert-butyl ester

生成物 1

HCID 58700383HCID 58700383、化合物

実験手順

The title compound was prepared by following the general method for (5-methyl-6-trifluoromethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indol-8-yl)-pyridin-3-yl-amine (Method A) as an oil (25 mg, 13%) from (4aS,9bR)-8-bromo-6-cyano-5-methyl-1,3,4,4a,5,9b-hexahydro-pyrido[4,3-b]indole-2-carboxylic acid tert-butyl ester (Example 158, 196 mg, 0.5 mmol), 6-trifluoromethyl-pyridin-3-ylamine (141 mg, 1.5 mmol) and NaOt-Bu (144 mg, 1.5 mmol). MS (ESI): 374 (base, M+H).

出典と根拠

ORDレコード: ord-3d4f48aca97244ceab7a02916be7efcc
出典データセット: uspto-grants-2006_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07109339B2

反応ノート

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