- Preparation method of R-N-Boc-3-pyrrolidine acetic acid
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The invention provides a preparation method of R-N-Boc-3-pyrrolidine acetic acid, which comprises the following steps: by using N-Boc-3-pyrrolidone and trimethyl phosphonyl acetate as raw materials, carrying out wittig reaction, asymmetric reduction hydrogenation reaction and hydrolysis reaction to obtain the R-N-Boc-3-pyrrolidine acetic acid. The preparation method starts from a low-price racemicmixture N-Boc-3-pyrrolidone, the reaction conditions are mild, use of dangerous materials is not needed, the reaction steps are few, the process is simple, the single product R-N-Boc-3-pyrrolidine acetic acid with a target chiral structure can be finally obtained, the product has high purity, an optical activity ee value of more than 99% and high yield, and industrial scale-up production is facilitated.
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- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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- FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
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- ARYLVINYLAZACYCLOALKANE COMPOUNDS FOR CONSTIPATION
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The present invention relates to methods of treating constipation and enhancing colonic motility by administration of 5-((E)-2 pyrrolidin-3-ylvinyl)pyrimidine or a pharmaceutically acceptable salt thereof.
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- NOVEL COMPOUNDS
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The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, novel chemical compounds useful as intermediates, pharmaceutical compositions containing the product compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
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- SYNTHESIS AND NOVEL SALT FORMS OF (R)-5-((E)-2-(PYRROLIDIN-3-YLVINYL)PYRIMIDINE
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The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
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- Acetic acid derivatives
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Acetic acid derivatives of the formula STR1 wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
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