반응식
Cl.C([O:4][C:5](=[O:24])[CH2:6][O:7][C:8]1[CH:13]=[CH:12][C:11]([Cl:14])=[CH:10][C:9]=1[CH:15]1[C:20]2[S:21][CH:22]=[N:23][C:19]=2[CH2:18][CH2:17][NH:16]1)C.CCN(CC)CC.[CH3:32][O:33][C:34]1[CH:43]=[CH:42][CH:41]=[CH:40][C:35]=1[CH2:36][N:37]=[C:38]=[S:39].[OH-].[Na+]>CC#N.C(O)=O>[Cl:14][C:11]1[CH:12]=[CH:13][C:8]([O:7][CH2:6][C:5]([OH:4])=[O:24])=[C:9]([CH:15]2[C:20]3[S:21][CH:22]=[N:23][C:19]=3[CH2:18][CH2:17][N:16]2[C:38](=[S:39])[NH:37][CH2:36][C:35]2[CH:40]=[CH:41][CH:42]=[CH:43][C:34]=2[O:33][CH3:32])[CH:10]=1참가 물질
7
반응물 4
생성물 1
시약·촉매·용매 2
실험 절차
To a solution of (±)-[4-chloro-2-(4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridin-4-yl)-phenoxy]-acetic acid ethyl ester hydrochloride (50 mg, 0.13 mmol, 1.00 eq.) and NEt3 (54 μL, 0.39 mmol, 3.00 eq.) in MeCN (1 mL), 2-methoxybenzyl isothiocyanate (24 mg, 0.14 mmol, 1.05 eq.) in MeCN (1 mL) was added. The mixture was stirred at r.t. for 18 hours. 1M aq. NaOH (0.5 mL) was added. The mixture was stirred at r.t. for 18 hours. The solution was neutralized with formic acid, purified by prep. HPLC (column: Atlantis, 30×75 mm, 10 um, UV/MS, acidic conditions), and concentrated in vacuo to give the desired acid as a white solid.
후처리
- stirringThe mixture was stirred at r.t. for 18 hours
- custompurified by prep
- concentrationHPLC (column: Atlantis, 30×75 mm, 10 um, UV/MS, acidic conditions), and concentrated in vacuo
출처 및 근거
- ORD 기록
- ord-c0b01d7c0be74736aacdc50b232042f4
- 출처 데이터셋
- uspto-grants-2015_10
- 특허 번호
- US09169270B2
연결된 노트
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