- Synthesis method of N-cyclohexyl-5-(4-chlorobutyl)-1H-tetrazole
-
The invention discloses a synthesis method of N-cyclohexyl-5-(4-chlorobutyl)-1H-tetrazole. The synthesis method comprises the following steps: firstly, synthesizing N, N-dimethylformamide; the synthesis method comprises the following synthesis steps: taking 5-chlorovaleronitrile and cyclohexanol as raw materials, controlling the molar ratio of the 5-chlorovaleronitrile to the cyclohexanol to be (1: 1)-(1: 1.5) and the reaction temperature to be 5-55 DEG C, and carrying out a catalytic reaction for 1-6 hours by virtue of concentrated sulfuric acid, so as to obtain 5-chloro-N-cyclohexylvaleramide; wherein the molar ratio of the 5-chlorovaleronitrile to the concentrated sulfuric acid for catalysis is (1: 3)-(1: 10); the preparation method comprises the following steps: treating 1, 5-chloro-N-cyclohexylvaleric amide with phosphorus pentachloride; wherein the molar ratio of the 3, 5-chloro-N-cyclohexylvaleric amide to the phosphorus pentachloride is (1: 1)-(1: 1.5) and the molar ratio of the 2, 5-chloro-N-cyclohexylvaleric amide to the phosphorus pentachloride is (1: 1)-(1: 1.5); according to the invention, trimethyl silicon azide is used as a cyclization reagent instead of azoic acid or sodium azide, so that the synthesis method has the advantages of higher stability, no explosion and higher safety, the cost can be effectively reduced, the synthesis method is environment-friendly,and the purity of the obtained product is high.
- -
-
Paragraph 0012-0014
(2020/06/20)
-
- CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
-
The present invention discloses compounds of Formula I: (I) having 11beta -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
- -
-
Page/Page column 79-80
(2008/06/13)
-
- CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
-
The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention compositions containing these compounds for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula I wherein G1 is methylene or ethylene; L is-(C1-C4)alkylene-, -S-, -CH(OH)-, or -O-; R0 is Formula II or Formula III and the other substituents are as defined in the claims.
- -
-
Page/Page column 53
(2008/06/13)
-
- Imidazopyridine derivatives and pharmaceutical compositions
-
This invention relates to novel imidazopyridine derivatives useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention further relates to pharmaceutical compositions of such imidazopyridine derivatives.
- -
-
-
