专利号:US-7714063-B2 优先权日:2007-11-15 标 题 :Solid support for Fmoc-solid phase synthesis of peptides 发明人:SRIVASTAVA KRIPA SHANKER; DAVIS MATTHEW RYAN 权利人:MALLINCKRODT INC 摘要:The present invention provides compositions and processes for the solid phase synthesis of polypeptides. In particular, the present invention provides solid supports and processes for preparing solid supports for the synthesis of polypeptides.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:WO-2008105759-A1 优先权日:2007-02-27 标 题:Methods for synthesis of modified peptides 发明人:BROWER JUSTIN O 权利人:ARGOLYN BIOSCIENCE INC; BROWER JUSTIN O 摘要:Methods for the synthesis of peptides and peptide analogs containing aminoacid residues bearing substituted amino- and guanido- sidechains, such as alkyl lysine and arginine residues, are provided.
专利号:US-9556140-B2 优先权日:2013-01-26 标 题 :Approach for synthesis of catechins 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; RAI KUMAR SANTOSH; TRIPATHI VINAYAK; PATIL ISHWAR RAKESH 权利人:SPHAERA PHARMA PRIVATE LTD 摘要:A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.
专利号:US-7825257-B1 优先权日:2007-10-23 标题 :Synthesis of benzotriazole monomer 发明人:DEO KESHAV; SHAH CHANDRAKANT CHUNILAL; PATEL KALPESH; PATEL NILPESH; PAREKH VIRAL; PATEL RONAK; SONI JIGNESH; SHAH HIRAL; SEELYE DAVID E; NANDU MAHENDRA P 权利人:BAUSCH & LOMB 摘要:The synthesis of benzotriazole monomers and the use of the benzotriazole monomers and one or more other monomers to prepare ultraviolet (UV) light absorbing polymer compositions. The synthetic methods described in this application provide a significant improvement over the previous methods used to prepare benzotriazole monomers.
专利号:US-6455680-B1 优先权日:2000-12-21 标 题 :Methods utilizing aryl thioimines in synthesis of erythromycin derivatives 发明人:LUKIN KIRILL A 权利人:ABBOTT LAB 摘要:An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.