3-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acid → 3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carboxylic acid [1-(5-fluoro-6-methoxy-3,4-dihydro-2H-1-oxa-9-aza-phenanthren-3-ylmethyl)-piperidin-4-yl]-amide

HRID 633830ノート

反応式

HRID 633830 の反応式
Br[CH2:2][CH:3]1[CH2:16][C:15]2[C:14]3[C:9](=[CH:10][CH:11]=[C:12]([O:18][CH3:19])[C:13]=3[F:17])[N:8]=[CH:7][C:6]=2[O:5][CH2:4]1.C(OC([N:27]1[CH2:32][CH2:31][CH:30]([NH2:33])[CH2:29][CH2:28]1)=O)(C)(C)C.[O:34]=[C:35]1[NH:40][C:39]2[CH:41]=[C:42]([C:45](O)=[O:46])[CH:43]=[CH:44][C:38]=2[S:37][CH2:36]1>>[F:17][C:13]1[C:12]([O:18][CH3:19])=[CH:11][CH:10]=[C:9]2[C:14]=1[C:15]1[CH2:16][CH:3]([CH2:2][N:27]3[CH2:28][CH2:29][CH:30]([NH:33][C:45]([C:42]4[CH:43]=[CH:44][C:38]5[S:37][CH2:36][C:35](=[O:34])[NH:40][C:39]=5[CH:41]=4)=[O:46])[CH2:31][CH2:32]3)[CH2:4][O:5][C:6]=1[CH:7]=[N:8]2

参加物

4

反応物 3

HCID 7609933-oxo-3,4-dihydro-2H-1,4-benzothiazine-6-carboxylic acidHCID 12682914-Amino-1-Boc-piperidineHCID 867307103-bromomethyl-5-fluoro-6-methoxy-3,4-dihydro-2H-1-oxa-9-aza-phenanthrene

生成物 1

HCID 714755253-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carboxylic acid [1-(5-fluoro-6-methoxy-3,4-dihydro-2H-1-oxa-9-aza-phenanthren-3-ylmethyl)-piperidin-4-yl]-amide

実験手順

The titled compound is prepared as a white lyophilized powder following Scheme 1 and in analogy to Example 1 using 3-bromomethyl-5-fluoro-6-methoxy-3,4-dihydro-2H-1-oxa-9-aza-phenanthrene, 4-amino-piperidine-1-carboxylic acid tert-butyl ester and 3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carboxylic acid as starting material.

出典と根拠

ORDレコード
ord-cbfae806eea648a491e560457c6dc52f
出典データセット
uspto-grants-2016_04
特許番号
US09321788B2

反応ノート

読み込み中…