专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 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 programs. 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 preorganising 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-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-2004058888-A1 优先权日:2000-01-13 标题:Methods for synthesis of alpha-d-gal (1~>3) gal-containing oligosaccharides 发明人:BORNAGHI LAURENT; DEKANY GYULA; DRINNAN NICHOLAS BARRY; PAPAGEORGIOU JOHN; WEST MICHAEL LEO 摘要:This invention relates to reagents and methods for synthesis of biologically active di- and tri-saccharides comprising α-D-Gal(1→3)-D-Gal. In particular the invention provides novel reagents, intermediates and processes for the solution or solid phase synthesis of α-D-galactopyranosyl-(1→3)-D-galactose, and derivatives thereof. In one preferred embodiments the invention provides a protected monosaccharide building block of general formula (II): in which R 3 is methoxy or methyl; R 1 is H, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4-chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl; and R 2 is H, Fmoc, benzoyl, pivaloyl, 4-chlorobenzoyl, acetyl, chloroacetyl, levulinoyl, 4-methylbenzoyl, benzyl, 3,4-methylenedioxybenzyl, 4-methoxybenzyl, 4 -chlorobenzyl, 4-acetamidobenzyl, or 4-azidobenzyl.
专利号:US-7973171-B2 优先权日:2005-06-13 标题:Process for synthesis of dialkoxyorganoboranes 发明人:BURKHARDT ELIZABETH; ATKINS WILLIAM 权利人:BURKHARDT ELIZABETH; ATKINS WILLIAM 摘要:The invention relates to a process for the synthesis of dialkoxyorganoboranes, in particular to a process for the synthesis of dialkoxyorganoboranes by an ester exchange reaction. Moreover, the invention relates to a process for the synthesis of organo-oxazaborolidine catalysts (organo-CBS) and of trialkylboroxins. Furthermore, the invention relates to methods of using dialkoxyorganoboranes for the preparation of organo-CBS catalysts and in Suzuki-type coupling reactions.
专利号:US-2012165520-A1 优先权日:2010-12-23 标题:Process for the synthesis of prodrugs of opioids 发明人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 权利人:MCGEE PAUL; GARNETT IAN; JUAN E; MANAGE A; CARNIAUX JEAN-FRANCOIS 摘要:The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
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