- TETRAHYDROCARBAZOLE DERIVATIVES USEFUL AS ANDROGEN RECEPTOR MODULATORS
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The present invention provides a compound of the formula: Formula I or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or ex
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Page/Page column 142-143
(2010/11/25)
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- 2-CHLORO-1,3-THIAZOLE-5-METHANOL DERIVATIVE, ITS MANUFACTURING METHOD AND AGRICULTURAL/HORTICULTURAL DISEASE-CONTROLLING AGENT
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PROBLEM TO BE SOLVED: To provide a novel compound exhibiting excellent effects of controlling various plant diseases, a synthesizing method of the compound and an agrochemical comprising as the effective ingredient a 2-chloro-1,3-thiazole-5-methanol derivative, particularly a plant disease-controlling agent. SOLUTION: The 2-chloro-1,3-thiazole-5-methanol derivative is represented by formula (I) [wherein R is a hydrogen atom, an optionally substituted 1-4C alkyl group, a 3-6C alkenyl group, a (cyano) 1-4C alkyl group, an optionally substituted tetrahydropyranyl group, an optionally substituted carbonyl group, an optionally substituted phenyl group or an optionally substituted sulfonyl group]. The manufacturing method of the compound and the agricultural/horticultural disease-controlling agent comprising the compound as the effective ingredient are also provided.
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Page/Page column 8
(2010/02/11)
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- Intermediate thiazoles and process for the preparation of 2-chloro-5-chloromethyl-thiazole
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The present invention relates to intermediate thiazole compounds and a process for preparing 2-chloro-5-chloromethylthiazole which is a known compound useful for the preparation of insecticides.
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- Process for the preparation of thiazole derivatives
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A process for the preparation of a compound of formula (I), wherein X is a leaving group; which process comprises, a) for the preparation of a compound of formula (I) wherein X is —OS(═O)2A and A is as defined in the specification, reacting a compound of formula (II) with a sulfonylating agent; or, b) for the preparation of a compound of formula (I) wherein X is iodine, reacting a compound of formula (III) with an iodinating agent, preferably sodium iodide; or, c) for the preparation of a compound of formula (I) whrein X is bromine, reacting a compound of formula (IV) with a brominating agent; or, d) for the preparation of a compound (I) wherein X is chlorine or bromine, reacting a compound (V), wherein R and X are as defined in the specification, with a chlorinating agent, a compound of formula (Ib), the use thereof and a process for the preparation of a compound of formula (II) and a compound of formula (A) are described.
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- Process for the preparation of 5-hydroxymethylthiazoles
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The present invention discloses a process for the preparation of a hydroxymethylthiazole compound having formula 3: The process of the invention comprises reacting a halomethyl thiazole having the formula: STR1 with water, at an elevated temperature. Optionally, the reaction can be carried out in the presence of a base, such as sodium carbonate, which can react with any acid formed. In the process of the invention, X is a halogen atom; and R6 is selected from the group consisting of hydrogen, and halogen atoms. The invention also contemplates the preparation of acid addition salts of the hydroxymethylthiazole, compound 3.
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- Process for preparation of 5-hydroxymethylthiazole
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A process for the preparation of 5-hydroxymethylthiazole comprises reacting a compound of the formula, STR1 with a carboxylic acid salt (optimally in the presence of a quaternary ammonium salt) and hydrolyzing the resulting ester. Subsequent dechlorination gives 5-hydroxymethylthiazole.
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- Process for the preparation of disubstituted carbonates
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The present invention relates to a process for the preparation of cabonate compounds useful for the preparation of compounds which are human immunodeficiency virus (HIV) protease inhibitors. The compounds have formula I: STR1 wherein R9 is hydrogen or lower alkyl, and the thiazolyl ring can be unsubituted or substituted with a lower alkyl group.
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