1246960-23-5Relevant academic research and scientific papers
Intermediate of Sitagliptin and synthesis method of intermediate
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Paragraph 0054; 0057-0060; 0070; 0071; 0078; 0092; 0093, (2017/07/19)
The invention provides an intermediate of Sitagliptin and a synthesis method of the intermediate. The intermediate is the compound of formula (I), and the synthesis method comprises enabling the compound of the formula (3) to react with cyan-containing salt to obtain the compound of the formula (2), and hydrolyzing the compound of the formula (2) by use of alkali. The synthesis method is short in reaction path, the reaction reagent is cheap, and the expensive reagent in the traditional process is avoided to use, the production cost can be effectively lowered, the synthesis time is shortened, and the industrial production is facilitated. The intermediate of the Sitagliptin manufactured by use of the synthesis method is large in yield, high in purity, and in favor of the preparation of high-quality Sitagliptin.
A concise enantioselective synthesis of (R)-selegiline, (S)-benzphetamine and formal synthesis of (R)-sitagliptin via electrophilic azidation of chiral imide enolates
Dey, Soumen,Sudalai, Arumugam
, p. 67 - 72 (2015/02/02)
A concise and high yielding enantioselective synthesis of (R)-selegiline, an anti-Parkinson's drug, (S)-benzphetamine, an anti-obesity agent, and (S)-sitagliptin, an anti-diabetic drug has been described starting from commercially available starting materials employing Evans' electrophilic azidation of chiral imide enolates as a key chiral inducing step, which proceeds in a highly diastereoselective manner (>99%).
METHOD FOR PREPARING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE
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, (2012/02/01)
The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
