89874-51-1Relevant articles and documents
Method for asymmetrically synthesizing (S)-preclamol
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, (2019/02/04)
The invention discloses a novel method for asymmetrically synthesizing (S)-preclamol. The method comprises the following steps: using racemic alpha-halogenated glutaric acid diester as a starting material to be subjected to an asymmetric Negishi cross-coupling reaction with zinc m-methoxyphenyl bromide under the catalysis of a bisoxazoline chiral ligand and metal cobalt to obtain m-methoxyphenyl-substituted glutaric acid diester, then reducing by LiAlH4 to form (S)-2-(3-methoxyphenyl) pentanediol, and finally performing to amination cyclization and desmethylation to obtain (S)-preclamol. The asymmetric Negishi cross-coupling reaction is utilized for the first time to directly construct the chiral center of (S)-preclamol, the synthesis route is short, the reaction conditions are mild, and the total yield is 51%.
Stereoselective synthesis of (?)-3-PPP through palladium-catalysed unactivated C(sp3)–H arylation at the C-3 position of L-pipecolinic acid
Zhang, Shi-Jin,Sun, Wen-Wu,Yu, Qun-Ying,Cao, Pei,Dong, Xiao-Ping,Wu, Bin
, p. 606 - 609 (2017/01/25)
An efficient route for the preparation of (?)-3-PPP(preclamol) using the highly stereoselective palladium-catalysed C(sp3)-H arylation and radical decarboxylation reaction as the key steps is described. The chiral center at the C-3 position of
N-OXIDE AND/OR DI-N-OXIDE DERIVATIVES OF DOPAMINE RECEPTOR STABILIZERS/MODULATORS DISPLAYING IMPROVED CARDIOVASCULAR SIDE-EFFECTS PROFILES
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Page/Page column 25-26, (2008/12/08)
The invention relates to N-oxide and/or di-N-oxide derivatives of dopamine receptor stabilizers/modulators having the general formula (1) or (2) and pharmaceutical preparations containing the said compounds. Further, the invention relates the use of the s