83124-74-7Relevant articles and documents
C-Bridged Bispyrrolidines and Bispiperidines as New Ligands
Stumpf, Tim-Daniel J.,Steinbach, Manfred,H?ltke, Magdalene,Heuger, Gerold,Grasemann, Franka,Fr?hlich, Roland,Schindler, Siegfried,G?ttlich, Richard
, p. 5538 - 5547 (2018/10/25)
The preparation of methylene-bridged C2-symmetric nitrogen-heterocycles as a new class of ligands is described, including methylene-bridged pyridines, quinolones, piperidines and pyrrolidines. These methylene-bridged aromatic systems are obtained via a microwave assisted Ziegler-type reaction. The separation of diastereomers and the application of the copper complexes of these ligands for cyclopropanation reactions proves the applicability of these new types of ligands.
Preparation method of 3,3-dialkoxylpropionate
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Paragraph 0023; 0024, (2017/09/02)
The invention belongs to the technical field of preparation of drug intermediates and in particular relates to a preparation method of 3,3-dialkoxylpropionate. The preparation method comprises the following steps: firstly, taking alkyl vinyl ether and trichloroacetyl chloride as raw materials; reacting under a certain condition to obtain an intermediate product 1,1,1-trichloro-4-alkoxyl-3-butene-2-one; reacting under an alkaline condition to obtain a target product 3,3-dialkoxylpropionate. The preparation method of the 3,3-dialkoxylpropionate, provided by the invention, has the following active effects that one raw material is directly used as a solvent (trichloroacetyl chloride) to react and the recycling and consumption of the solvent in a production process are reduced to a certain extent; after the reaction, an alcohol solvent can be recycled and is used for reacting for the next time, so that the recycling is realized and the scheme meets the requirements of green chemistry; a preparation process is simple, low in energy consumption and low in cost and can be in mass production.
A method for synthesizing allah Geleg sandbank (by machine translation)
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Paragraph 0010, (2016/10/10)
The invention relates to a method for preparing anti-II type diabetes drug allah Geleg sandbank method for the synthesis of bulk drug (Anagliptin). The lack of commercial synthetic allah Geleg sandbank solve the technical problems of the method. Synthetic method comprises the following steps : (1) with vinyl ether and trichloro acetyl chloride as the raw material, passes through the three-step reaction to obtain the aldehyde protected intermediates 4 ; The 3-amino-5-methyl pyrazole condensation for dehydrating and gets pyrazolo pyrimidine mother nucleus; Carboxy b ester hydrolysis to obtain 2-methyl-pyrazolo [1,5-a] pyrimidin 6-carboxylic acid 6 ; (2) to L-proline as a raw material, passes through the methyl esterification, ammoniation, acetylation, Carbonitride reaction to obtain the chiral cyano pyrrolizinone intermediate 11 ; Chiral cyano pyrrolizinone intermediate 11 And diamine fragment 12 In alkaline conditions to obtain intermediate affinity substituted 13 ; Finally, intermediate 13 Under the conditions of the hydrochloric acid removal protection Boc base namely obtain cyanopentanoyl Azolylamine intermediate 14 ; (3) 2-methyl-pyrazolo [1,5-a] pyrimidine-6-carboxylic acid 6 The cyano Azolylamine intermediate 14 The condensation conditions to obtain the bulk drug allah Geleg sandbank coupled. (by machine translation)