专利号:WO-9964428-A1 优先权日:1998-06-10 标题:Synthesis of aryl boronic acids 发明人:SULLIVAN JEFFREY M; BARNES HAMLIN H 权利人:BOULDER SCIENT CO; SULLIVAN JEFFREY M; BARNES HAMLIN H 摘要:A method for synthesis of aryl boronic acids is disclosed.
专利号:US-7193077-B2 优先权日:2003-08-30 标 题 :Exocyclic amine triaryl methyl protecting groups in two-step polynucleotide synthesis 发明人:DELLINGER DOUGLAS J; SIERZCHALA AGNIESZKA B; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC 摘要:Precursors for use in the synthesis of polynucleotides and methods of using the precursors in synthesizing polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group.
专利号:US-7427679-B2 优先权日:2003-08-30 标 题:Precursors for two-step polynucleotide synthesis 发明人:DELLINGER DOUGLAS J; SIERZCHALA AGNIESZKA B; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC 摘要:Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group. In particular embodiments, the precursor has the structure: n nwherein:n O and H represent oxygen and hydrogen, respectively, R 1 is hydrido, hydroxyl, protected hydroxyl, lower alkyl, modified lower alkyl, or alkoxy, one of R 2 or R 3 is a hydroxyl protecting group; and the other of R 2 or R 3 is a reactive group capable of reacting with a reactive site hydroxyl, Base is a heterocyclic base having an exocyclic amine group, and Tram is a triaryl methyl group having the structure (V) n nwherein the broken line represents a bond to the amino nitrogen of the exocyclic amine group, and R 4 , R 5 and R 6 are independently selected from unsubstituted or substituted aryl groups, provided that at least one of R 4 , R 5 , and R 6 is an aryl group other than phenyl and other than substituted phenyl.
专利号:WO-2012089181-A1 优先权日:2010-12-30 标题 :O-substituted (2r,3r)-3-(3-hydroxyphenyl)-2-methyl-4-pentenoic acids and a method of obtaining the same 发明人:VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 权利人:ZENTIVA KS; VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 摘要:The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.
专利号:WO-2014011120-A1 优先权日:2012-07-13 标 题 :Endoperoxides, synthesis and uses thereof for the treatment of neoplastic diseases such as cancer 发明人:TAN NGUAN SOON; CHIBA SHUNSUKE 权利人:UNIV NANYANG TECH 摘要:The present invention generally relates to processes and methods for the synthesis of endoperoxide compounds. More specifically, the invention relates to a method for preparing endoperoxide compounds starting from an aryl imine of formula (I) in the presence of a metallic catalyst and oxygen. The present invention also relates to endoperoxide compounds of formula (III) and their pharmaceutically acceptable salts thereof, useful for therapy. All substituents are defined herein. Also disclosed are methods of treating cancer using the compounds of formula (III).
专利号:US-7417139-B2 优先权日:2003-08-30 标 题 :Method for polynucleotide synthesis 发明人:DELLINGER DOUGLAS J; SIERZCHALA AGNIESZKA B; CARUTHERS MARVIN H; DELLINGER GERALDINE F 权利人:AGILENT TECHNOLOGIES INC 摘要:Methods of forming an internucleotide bond are disclosed. Such methods find use in synthesis of polynucleotides. The method involves contacting a functionalized support with a precursor having an exocyclic amine triaryl methyl protecting group under conditions and for a time sufficient to result in internucleotide bond formation. The functionalized support includes a solid support, a triaryl methyl linker group, and a nucleoside moiety having a reactive site hydroxyl, the nucleoside moiety attached to the solid support via the triaryl methyl linker group. In particular embodiments, the precursor has the structure: n nwherein:n O and H represent oxygen and hydrogen, respectively R1 is hydrido, hydroxyl, protected hydroxyl, lower alkyl, modified lower alkyl, or alkoxy, one of R2 or R3 is a hydroxyl protecting group; and the other of R2 or R3 is a reactive group capable of reacting with the reactive site hydroxyl, Base is a heterocyclic base having an exocyclic amine group, and Tram is the exocyclic amine triaryl methyl protecting group.
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 599. 摘要:Hari, Y.; Aoyama, T.; Shioiri, T., Science of Synthesis Knowledge Updates, (2010) 4, 30. 摘要:Okamoto, K.; Ohe, K., Science of Synthesis Knowledge Updates, (2020) 1, 142. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 188. 摘要:Clark, R. W.; Wiskur, S. L., Science of Synthesis Knowledge Updates, (2015) 1, 10.