专利号:US-8642809-B2 优先权日:2007-09-25 标 题:Methods of synthesis of certain hydroxamic acid compounds 发明人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S 权利人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S; TOPOTARGET UK LTD 摘要:The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PUR C ) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PUR E ) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PUR F ) optional purification; (HAF) hydroxamic acid formation; and (PUR G ) optional purification.
专利号:US-8703952-B2 优先权日:2008-12-12 标题:Synthesis of 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline and analogues and intermediates 发明人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID 权利人:WILLIAMSON CRAIG; STOREY JOHN MERVYN DAVID; WISTA LAB LTD 摘要:The present invention pertains generally to methods of preparing certain 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds and their analogues, and especially to methods of preparing dimebon. The present invention also pertains to methods of preparing certain intermediate compounds which find use in the synthesis of the 9-(arylalkyl)-1,2,3,4-tetrahydro-γ-carboline compounds.
专利号:US-7557099-B2 优先权日:2004-03-01 标题 :Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines 发明人:HOWARD PHILIP WILSON; KANG GYOUNG-DONG 权利人:SPIROGEN LTD 摘要:Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R 2 and R 3 are independently selected from —H, â•?O, â•?CH 2 , —CN, —R, OR, halo, â•?CH—R, O—SO 2 —R, CO 2 R and COR; R 10 is a carbamate-based nitrogen protecting group; and R 11 is an oxygen protecting group.
专利号:US-4620015-A 优先权日:1981-12-28 标题:Synthesis of β-((2-methylpropoxy)methyl)-N-phenyl-N-(phenylmethyl)-1-pyrrolidineethanamine 发明人:STIEFEL FRANK J 权利人:CARTER WALLACE 摘要:A novel, efficient, economical procedure for the synthesis of ethers of n-propanoldiamine having the formula: ##STR1## wherein R is a straight or branched chain lower alkyl group or an aralkyl group, Ar is an aromatic group, Ar 1 is an aromatic or heterocyclic group, A is a tertiary aliphatic, cycloaliphatic or heterocyclic amino group and addition salts thereof with pharmacologically acceptable acids.
专利号:US-2013012706-A1 优先权日:2010-03-01 标 题 :Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines 发明人:HUMMERSONE MARC GEOFFERY; COUSIN DAVID 权利人:PHARMINOX LTD; HUMMERSONE MARC GEOFFERY; COUSIN DAVID 摘要:The present invention provides a compound of general formula (II), or a salt or solvate thereof: n n n n n n n n n n n n wherein n A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein:n -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate;n nand its use in the synthesis of temozolomide and analogues thereof.
专利号:US-11897914-B2 优先权日:2021-11-29 标题 :Synthesis of 2′ protected nucleosides 发明人:POON WING C; ZOU RUIMING; LAU ALDRICH N K; YU DAVID; Du Gengyu; YAO YUN-CHIAO; ZHAO GANG 权利人:HONGENE BIOTECH CORP 摘要:Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.
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合成参考文献
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