{(S)-6-[(R)-4-Bromomethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester → {(S)-6-[(R)-4-(7,8-Dihydro-pyrido[4,3-d]pyrimidin-6-ylmethyl)-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester

反応式

[CH3:1][O:2][C:3](=[O:30])[CH2:4][C@H:5]1[C:9]2[CH:10]=[CH:11][C:12]([O:14][C@H:15]3[C:23]4[C:18](=[C:19]([CH2:28]Br)[C:20]([C:24]([F:27])([F:26])[F:25])=[CH:21][CH:22]=4)[CH2:17][CH2:16]3)=[CH:13][C:8]=2[O:7][CH2:6]1.[N:31]1[C:36]2[CH2:37][CH2:38][N:39](C[B-](F)(F)F)[CH2:40][C:35]=2[CH:34]=[N:33][CH:32]=1>>[CH3:1][O:2][C:3](=[O:30])[CH2:4][C@H:5]1[C:9]2[CH:10]=[CH:11][C:12]([O:14][C@H:15]3[C:23]4[C:18](=[C:19]([CH2:28][N:39]5[CH2:38][CH2:37][C:36]6[N:31]=[CH:32][N:33]=[CH:34][C:35]=6[CH2:40]5)[C:20]([C:24]([F:27])([F:26])[F:25])=[CH:21][CH:22]=4)[CH2:17][CH2:16]3)=[CH:13][C:8]=2[O:7][CH2:6]1

参加物

反応物 2

HCID 86700813{(S)-6-[(R)-4-Bromomethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester

HCID 131732226(7,8-Dihydro-pyrido[4,3-d]pyrimidin-6-yl)methyltrifluoroborate

生成物 1

HCID 90313477{(S)-6-[(R)-4-(7,8-Dihydro-pyrido[4,3-d]pyrimidin-6-ylmethyl)-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester

実験手順

The title compound is prepared from {(S)-6-[(R)-4-bromomethyl-5-trifluoromethyl-indan-1-yloxy]-2,3-dihydro-benzofuran-3-yl}-acetic acid methyl ester and (7,8-dihydro-pyrido[4,3-d]pyrimidin-6-yl)methyltrifluoroborate following a procedure analogous to that described for Intermediate 3. LC (method 1): tR=1.13 min; Mass spectrum (ESI+): m/z=540 [M+H]+.

出典と根拠

ORDレコード: ord-484b3f66e95a48c8ae44604e92623a6d
出典データセット: uspto-grants-2015_01
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08927531B2

反応ノート

読み込み中…