专利号:US-2008214637-A1 优先权日:2004-11-11 标题 :Process for the Synthesis of Tetrazoles 发明人:ANTONCIC LJUBOMIR; LUDESCHER JOHANNES 权利人:LEK PHARMACEUTICALS 摘要:A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.
专利号:US-5039814-A 优先权日:1990-05-02 标 题:Ortho-lithiation process for the synthesis of 2-substituted 1-(tetrazol-5-yl)benzenes 发明人:SHUMAN RICHARD F; KING ANTHONY O; ANDERSON ROBERT K 权利人:MERCK & CO INC 摘要:A process utilizes the tetrazole functional group to direct lithiation at the ortho position of a phenyltetrazole and generate a nucleophilic aryllithium species which then undergoes reaction with an electrophile to generate a 2-substituted 1-(tetrazol-5-yl)benzene. The process is useful in the production of intermediates in the synthesis of angiotensin II antagonists. This novel process is a more cost effective and versatile route for the large-scale preparation of these key intermediates.
专利号:US-6326498-B1 优先权日:2001-03-13 标 题 :Process for the synthesis of 5-(2-flurophenyl)-1H-tetrazole 发明人:MALLADI PARDHASARADHI; KANTEVARI SRINIVAS; NAIR CHEMBUMKULAM KAMALAKSHYAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses a process of the preparation of 5-(2-flurophenyl)-1H-tetrazole of the formula 2 by reacting 2-fluoro benzonitrile of the formula 1 n with an inorganic azide and an amine salt in an aromatic solvent, precipitating the product with hydrochloric acid and separating the precipitated product.
专利号:WO-2008012852-A1 优先权日:2006-07-27 标 题:Intermediate compounds for the preparation of angiotensin ii antagonists 发明人:GUANDALINI LUCA; MARTINI ELISABETTA; ROMANELLI MARIA NOVELLA; DALLATOMASINA FRANCO 权利人:S I M S S R L SOC IT MEDICINAL; GUANDALINI LUCA; MARTINI ELISABETTA; ROMANELLI MARIA NOVELLA; DALLATOMASINA FRANCO 摘要:The present invention relates to novel substituted biphenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists, to a process for the synthesis of them and to a process for the conversion thereof to said molecules.
专利号:WO-9637481-A1 优先权日:1995-05-26 标题:Novel reagent for tetrazole synthesis and process for producing tetrazoles therewith 发明人:TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 权利人:CHUGOKU KAYAKU; WAKUNAGA SEIYAKU KK; TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 摘要:A process for producing 1H-tetrazoles represented by general formula (II) (wherein R represents an arbitrary substituent) from carbonitriles represented by the general formula (I): R-CN (wherein R is as defined above) with the use of a tetrazolating agent comprising an alkali metal azide and zinc chloride. The agent can be used in a variety of solvents and can fundamentally be applied to any carbonitriles. As zinc chloride is inexpensive, it contributes to cost reduction.
专利号:US-5371233-A 优先权日:1991-12-30 标 题:2-(tetrazol-5-yl)-1,1'-biphenyl derivatives, their preparation and their use as synthetic intermediates 发明人:DAUMAS MARC; HOORNAERT CHRISTIAN; CHEKROUN ISAAC; BEDOYA-ZURITA MANUEL; RUIZ-MONTES JOSE; ROSSEY GUY; GRECIET HELENE 权利人:SYNTHELABO 摘要:Compounds corresponding to the formula (I) ##STR1## in which X represents dibromomethyl, formyl, (C 1-4 )alkyl, or a group CH(OR 5 ) 2 or CH(OH)OR 5 , wherein the or each R 5 is hydrogen (C 1-3 )alkyl or the two R 5 's in the case of CH(OR 5 ) 2 are linked to provide a 1,3-dioxolane or 1,3-dioxane ring, and Y represents hydrogen, 1,1-dimethylethyl, triphenylmethyl, trimethylstannyl, tributylstannyl, (1,1-dimethylethyl)dimethylsilyl, (1,1-dimethylethyl)diphenylsilyl, 2-cyanoethyl, or a group CH 2 OR 6 wherein R 6 is methyl, phenylmethyl, 1,1-dimethylethyl, 2,2,2-trichloroethyl, benzyloxycarbonyl or 2,2,2-trichloroethyloxycarbonyl, Y being in position 1 or 2 on the tetrazole ring. The compounds of formula (I) are useful as intermediates in the synthesis of compounds possessing therapeutic activity.