66937-93-7

Upstream product

• 4021-08-3 4-methylpicolinic acid 
• 71-41-0 pentan-1-ol 
• 123387-50-8 4-methylpiperidine-1-carboxylic acid tert-butyl ester 
• 162167-52-4 (2R-trans)-1-[(Phenylmethoxy)carbonyl]-4-methyl-2-piperidinecarboxylic acid, ethyl ester 
• 64-17-5 ethanol 

Downstream Products

• 74863-81-3 ethyl 1-α-(tert-butoxycarbonyl)-N^ω-nitro-L-arginyl>-4-methyl-2-piperidinecarboxylate 
• 4939-37-1 2-methylquinolizidine 
• 152134-77-5 4-amino-N-[1-(1H-benzimidazol-5-yl-methyl)-2-(2-carbethoxy-4-methyl-piperidin-1-yl)-2-oxo-ethyl]-3,5-dichloro-benzenesulphonamide 
• 131278-84-7 ethyl (2R,4R)-4-methyl-2-piperidinecarboxylate L-(+)-tartarate 
• 1401618-23-2 ethyl (2S,4S)-4-methyl-2-piperidinecarboxylate L-tartrate 
• 79199-62-5 ethyl (2S,4R)-4-methylpipecolate 
• 69129-28-8 ethyl 4-methyl-1-(N^ω-nitro-L-arginyl)piperidinecarboxylate hydrochloride 

Relevant academic research and scientific papers

Preparation method of argatroban intermediate esterified substance 4-methyl-2-ethyl piperidinecarboxylate

The invention relates to a preparation method of an argatroban intermediate esterified substance 4-methyl-2-ethyl piperidinecarboxylate. The preparation method comprises the following steps: adding a solvent, namely ethanol into a reaction kettle, putting a reactant, namely 4-methyl-2-piperidinecarboxylicacid hydrochloride into the reaction kettle, stirring to cool to (-5)-0 DEG C, maintaining the temperature, adding a catalyst, namely thionyl chloride, stirring to completely react until disappearance of raw material points is detected by virtue of a thin-layer chromatography, and carrying out vacuum reduced pressure concentration at 60 DEG C, so as to remove the solvent; and cooling the room temperature, adding dichloromethane, neutralizing reaction liquid by virtue of a 10% Na2CO3 solution, carrying out layered extraction, drying an organic solvent, and carrying out vacuum reduced pressure concentration at 50 DEG C on the organic solvent to remove the solvent, so as to obtain the esterified substance 4-methyl-2-ethyl piperidinecarboxylate. Mixed solvents including glacial acetic acid, ethanol and chloroform are replaced with single ethanol in a synthetic process, the reaction pressure is reduced, the catalyst thionyl chloride is low in cost, the operation is simple and convenient, the yield is substantially increased, and reaction solvents can be recycled, so that the preparation method is relatively beneficial to large-scale industrial production.

Preparation method for argatroban intermediate

The invention belongs to the technical field of medicine synthesis, and relates to a preparation method for argatroban intermediate, namely, 4-methyl-2-piperidinecarboxylate. The argatroban intermediate is generated through catalysis of ethyl alcohol in an atmosphere of carbon monoxide. According to the preparation method, reaction steps are reduced; the reaction yield is improved generally; a product is more stable and purer; raw materials which are liable to produce poison, and highly acidic and corrosive raw materials are not used, so that the environmental protection pressure is lightened; the used solvent, ethyl alcohol, is easy to recycle and utilize; reaction conditions are mild; an economic and feasible process route is provided for large-scale industrial production.

Direct diastereoselective synthesis of (±)-cis- and (±)-trans-4-methylpipecolic acid and derivatives

(±)-cis- or (±)-trans-4-Methylpipecolic acid and ester derivatives can be obtained directly by addition of electrophiles to α-lithiated N-Boc 4-methylpiperidine.

Scavenger assisted combinatorial process for preparing libraries of amides, carbamates and sulfonamides

This invention relates to a novel solution phase process for the preparation of amide, carbamate, and sulfonamide combinatorial libraries. These libraries have utility for drug discovery and are used to form wellplate components of novel assay kits.

HETEROCYCLIC THROMBIN INHIBITORS

Heterocyclic thrombin inhibitors are provided which have the structure STR1 wherein n, R, R 1, R 2, R 3, G, G x, R. sup.6', Ra, Xa, R 6, Rb, R 3, p, Q, A and R 4 are as defined herein.

HETEROAROMATIC AMINE THROMBIN INHIBITORS

Sulfonamide thrombin inhibitors are provided which have the structure STR1 including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R 1 and R 2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R 1 and R. sup.2 can be taken together with the N atom to which they are attached to form a 4-to 8-membered ring; R 3 is monocyclic heteroaryl; and R 4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.

N2 -arylsulfonyl-l-argininamides and the pharmaceutically acceptable salts thereof

N2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.