1151240-89-9Relevant academic research and scientific papers
Preparation method of phenyl crotonic acid ester compound
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Paragraph 0030; 0033-0034; 0056-0057; 0063-0070, (2021/05/19)
The invention relates to the technical field of organic synthesis, in particular to a preparation method of a phenyl crotonate compound, the preparation method comprises the following steps: S1, carrying out Willgerodt-Kindler reaction on an acetophenone
Preparation method of sitagliptin intermediate
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Paragraph 0050-0065, (2019/07/04)
The invention belongs to the field of organic synthesis, and particularly relates to a preparation method of a sitagliptin intermediate. The intermediate has a structure as shown in the specification,R1 and R2 are same as or different, and are hydrogen or
TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES SALTS, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 15; 16, (2016/10/08)
The present invention relates to (R)-7-[3-Amino-4-(2,4,5-trifluoro-phenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-carboxylic acid pharmaceutical salts, methods for their preparation, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as a dipeptidyl peptidase IV inhibitor.
SALTS OF TETRAHYDROIMIDAZO Y1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 8, (2012/02/04)
Pharmaceutical salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
TETRAHYDRO-IMIDAZO[1,5-a]PYRAZINE DERIVATIVES SALTS, PREPARATION METHODS AND MEDICINAL USE THEREOF
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Page/Page column 8, (2012/03/27)
Pharmaceutically acceptable salts of (R)-7-[3-amino-4-(2,4,5-trifluorophenyl)-butyryl]-3-trifluoromethyl-5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine-1-formic acid, their preparation methods, compositions containing the said pharmaceutical salts and their use as medicaments, especially as dipeptidyl peptidase IV (DPP-IV) inhibitors are disclosed.
Improved enzymatic syntheses of valuable β-arylalkyl-β-amino acid enantiomers
Tasnadi, Gabor,Forro, Enik,Fueloep, Ferenc
experimental part, p. 793 - 799 (2010/06/20)
The enantioselective (E~ 200) Burkholderia cepacia-catalysed hydrolyses of β-amino esters with H2O (0.5 equiv.) in t-BuOMe or in i-Pr2O at 45 °C are described. The enantiomers of biologically relevant β-arylalkyl-substituted β-amino acids, and especially (R)-3-amino-3-(2,4,5-trifluorophenyl)butanoic acid, the intermediate of the new antidiabetic drug sitagliptine, were prepared with high enantiomeric excesses (ee≥96%) and in good yields (≥42%). The Royal Society of Chemistry 2010.
TETRAHYDRO-IMIDAZOY1,5-A¨PYRAZINE DERIVATIVES, PREPARATION METHODS AND MEDICAL USES THEREOF
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Page/Page column 17, (2010/10/03)
Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula ( I ), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitor, wherein the substituents of formula ( I ) are defined as same as the description.
PREPARATION OF SITAGLIPTIN INTERMEDIATE
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Page/Page column 13, (2009/06/27)
Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.
