Methanesulfonic Acid → (2-Chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-{3-[6-(4-methyl-piperazin-1-yl)-pyridin-2-yloxy]-propyl}-amine dimesylate salt

HRID 902651ノート

反応式

HRID 902651 の反応式
[CH3:1][N:2]1[CH2:7][CH2:6][N:5]([C:8]2[N:13]=[C:12]([OH:14])[CH:11]=[CH:10][CH:9]=2)[CH2:4][CH2:3]1.[C:15]1([CH:21]([C:40]2[CH:45]=[CH:44][CH:43]=[CH:42][CH:41]=2)[CH2:22][N:23]([CH2:36][CH2:37][CH2:38]O)[CH2:24][C:25]2[CH:30]=[CH:29][CH:28]=[C:27]([C:31]([F:34])([F:33])[F:32])[C:26]=2[Cl:35])[CH:20]=[CH:19][CH:18]=[CH:17][CH:16]=1.OC1C=C(C=CC=1)CC1N(COCC)N=NN=1.BrCCCO.[CH3:68][S:69]([OH:72])(=[O:71])=[O:70]>ClCCl>[S:69]([OH:72])(=[O:71])(=[O:70])[CH3:68].[S:69]([OH:72])(=[O:71])(=[O:70])[CH3:68].[Cl:35][C:26]1[C:27]([C:31]([F:32])([F:33])[F:34])=[CH:28][CH:29]=[CH:30][C:25]=1[CH2:24][N:23]([CH2:22][CH:21]([C:15]1[CH:16]=[CH:17][CH:18]=[CH:19][CH:20]=1)[C:40]1[CH:45]=[CH:44][CH:43]=[CH:42][CH:41]=1)[CH2:36][CH2:37][CH2:38][O:14][C:12]1[CH:11]=[CH:10][CH:9]=[C:8]([N:5]2[CH2:4][CH2:3][N:2]([CH3:1])[CH2:7][CH2:6]2)[N:13]=1

参加物

7

反応物 5

HCID 6395Methanesulfonic AcidHCID 123083-Bromo-1-propanolHCID 577571173-[(2-Chloro-3-trifluoromethyl-benzyl)-diphenylethyl-amino]-propan-1-olHCID 688254685-(3-Hydroxy-benzyl)-ethoxymethyl-1,2,3,4-tetrazoleHCID 178480672HCID 178480672、化合物

生成物 1

HCID 86598286(2-Chloro-3-trifluoromethyl-benzyl)-(2,2-diphenyl-ethyl)-{3-[6-(4-methyl-piperazin-1-yl)-pyridin-2-yloxy]-propyl}-amine dimesylate salt

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

Following the procedure of Example 6(d), except 6-(4-methyl-piperazin-1-yl)-pyridin-2-ol and N-(2,2-Diphenylethyl)-N-(3-hydroxy-propyl)-N-(2-chloro-3-trifluoromethyl-benzyl)amine were used instead of 5-(3-hydroxy-benzyl)-ethoxymethyl-1,2,3,4-tetrazole and 3-bromo-propanol in step 6(d), the title compound was synthesized as the free base. The tertiaryamine was then dissolved in dichloromethane and two equivalents of methanesulfonic acid were added to afford the title compound as the dimesylate salt, 47 mg (19% yield), as a white solid. MS (ESI) 623.4 (M+).

後処理

  1. customthe title compound was synthesized as the free base

出典と根拠

ORDレコード
ord-69d7d342c37b44f9a7e3b40a2974405e
出典データセット
uspto-grants-2008_04
特許番号
US07365085B2

反応ノート

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