专利号:US-9840468-B1 优先权日:2016-12-30 标 题:Methods for the preparation of 6-aminoisoquinoline 发明人:CHAMBOURNIER GILLES; DELONG MITCHELL A 权利人:AERIE PHARMACEUTICALS INC 摘要:Described are methods for the preparation of 6-aminoisoquinoline, a useful intermediate compound in the synthesis of kinase inhibitors.
专利号:US-5969155-A 优先权日:1997-04-11 标题:Conversion of trinitrotoluene into high value compounds 发明人:ETURI SREENIVASA R; BASHIR-HASHEMI ABDOLLAH; IYER SURY 权利人:US ARMY 摘要:The present invention is directed to the synthesis of useful products from the explosive trinitrotoluene. This substance has a limited shelf life as a reliable explosive and large quantities of it have and will become surplus. Ecologically safe, and preferably commercially useful ways of disposing of it are therefore much to be desired. In the present invention the end products are nitroindoles of the general formula 4-Z 1 ,6-Z 2 indole wherein Z 1 and Z 2 are the same or different and are halo or nitro provided at least one of said groups is nitro.
专利号:US-7718598-B1 优先权日:1998-09-25 标 题:Auxiliary for amide bond formation 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programmes. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganizing peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-5786448-A 优先权日:1996-11-07 标题:Combinatorial libraries of cyclic urea and cyclic thiourea derivatives and compounds therein 发明人:NEFZI ADEL; OSTRESH JOHN M; HOUGHTEN RICHARD 权利人:TREGA BIOSCIENCES INC 摘要:The invention provides a rapid approach for combinatorial synthesis and screening of libraries of cyclic urea and cyclic thiourea compounds. The present invention further provides the compounds made by the combinatorial synthesis.
专利号:US-6809202-B2 优先权日:1996-11-07 标 题 :Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof 发明人:NEFZI ADEL; OSTRESH JOHN M; HOUGHTEN RICHARD A 权利人:TORREY PINES INST 摘要:The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
专利号:CN-104902994-B 优先权日:2012-11-06 标 题 :Direct Synthesis of Hydrogen Peroxide
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合成参考文献
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