반응식
[CH2:1]([O:3][C:4](=[O:18])[CH:5]([O:15][CH2:16][CH3:17])[CH2:6][C:7]1[CH:12]=[CH:11][C:10]([OH:13])=[C:9]([CH3:14])[CH:8]=1)[CH3:2].[CH:19]([C:22]1[CH:27]=[CH:26][C:25]([C:28]2[S:29][C:30]([CH3:36])=[C:31]([CH2:33][CH2:34]O)[N:32]=2)=[CH:24][CH:23]=1)([CH3:21])[CH3:20].COC(=O)CC(=O)C(Br)C.C(C1C=CC(C(N)=S)=CC=1)(C)C.C1(P(C2C=CC=CC=2)C2C=CC=CC=2)C=CC=CC=1.N(C(OCC)=O)=NC(OCC)=O>O1CCCC1>[CH2:1]([O:3][C:4](=[O:18])[CH:5]([O:15][CH2:16][CH3:17])[CH2:6][C:7]1[CH:12]=[CH:11][C:10]([O:13][CH2:34][CH2:33][C:31]2[N:32]=[C:28]([C:25]3[CH:24]=[CH:23][C:22]([CH:19]([CH3:20])[CH3:21])=[CH:27][CH:26]=3)[S:29][C:30]=2[CH3:36])=[C:9]([CH3:14])[CH:8]=1)[CH3:2]참가 물질
반응물 6
HCID 11776Triphenylphosphine
HCID 220568ethyl N-ethoxycarbonyliminocarbamate
HCID 20788314-(Propan-2-yl)benzene-1-carbothioamide
HCID 9815681Methyl 4-bromo-3-oxopentanoate
HCID 226474402-[2-(4-Isopropyl-phenyl)-5-methyl-thiazol-4-yl]-ethanol
HCID 22708451Ethyl 2-ethoxy-3-(4-hydroxy-3-methylphenyl)propanoate생성물 1
시약·촉매·용매 1
실험 절차
In analogy to the procedure described in example 1 d], [rac]-2-ethoxy-3-(4-hydroxy-3-methyl-phenyl)-propionic acid ethyl ester (example 4 c]) was reacted with 2-[2-(4-isopropyl-phenyl)-5-methyl-thiazol-4-yl]-ethanol (prepared from [rac]-4-bromo-3-oxo-pentanoic acid methyl ester [PCT Int. Appl. (2001), WO 01/79202] and 4-isopropyl-thiobenzamide in analogy to the procedures described in examples 12 a] and 12 b]) in tetrahydrofuran in the presence of triphenylphosphine and DEAD (diethyl azodicarboxylate) to yield [rac]-2-ethoxy-3-(4-{2-[2-(4-isopropyl-phenyl)-5-methyl-thiazol-4-yl]-ethoxy}-3-methyl-phenyl)-propionic acid ethyl ester, which was further saponified in analogy to the procedure described in example 4 e], to yield [rac]-2-ethoxy-3-(4-{2-[2-(4-isopropyl-phenyl)-5-methyl-thiazol-4-yl]-ethoxy}-3-methyl-phenyl)-propionic acid as light yellow solid.
후처리
- customdescribed in example 1 d
출처 및 근거
- ORD 기록
- ord-3df94e7f23584f7a900aa583d2c7b0c9
- 출처 데이터셋
- uspto-grants-2004_10
- 특허 번호
- US06809110B2
연결된 노트
불러오는 중…