📜2-Benzyloxycarbonylamino-Pentanedioic Acid Diethyl Ester置于palladium On Activated Charcoal 氢气体系中,化学反应生成谷氨酸二乙酯 参考文献:A Simple Modular Synthesis Of Pyridinoline A Collagen Cross-Link Of Biochemical Interest 标题:A Simple Modular Synthesis Of Pyridinoline A Collagen Cross-Link Of Biochemical Interest 摘要:A Simple Convergent Synthesis Of The Collagen Cross-Link Pyridinoline Starting From Glycine Is Reported. (C) 2003 Elsevier Ltd. All Rights Reserved. Doi:10.1016/s0957-4166(03)00400-2
专利号:US-5633373-A 优先权日:1989-07-07 标 题 :Enantioselective synthesis of antifolates 发明人:BARNETT CHARLES J; WILSON THOMAS M 权利人:LILLY CO ELI 摘要:A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
专利号:WO-2013164856-A1 优先权日:2012-05-04 标题 :A process for preparing intermediates of 10-propargyl-10-deazaaminopterin (pralatrexate) synthesis and the intermediates thereof 发明人:ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD 权利人:AVRA LAB PRIVATE LTD; ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD 摘要:A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaaminopterin (Pralatrexate) is obtained by peptide formation and ester hydrolysis of the intermediate compound 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid by methods known in the art.
专利号:US-8981090-B2 优先权日:2010-07-22 标 题:Process for the synthesis of pemetrexed disodium salt 发明人:CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO 权利人:CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO; CHEMI SPA 摘要:The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 n nby purifying the mixture obtainable by reacting compounds 1 and 1a in the presence of a chemical agent capable of promoting the formation of a peptide bond in an aprotic organic solventn n ncharacterized in that the mixture is subjected to the following steps:n a) washing with a basic aqueous solution; b) concentration of the organic phase; c) addition of a polar organic solvent and/or a mixture of polar organic solvents; d) precipitation of the pemetrexed diethyl ester 2.
专利号:US-5698556-A 优先权日:1995-06-07 标题 :Methotrexate analogs and methods of using same 发明人:CHAN CARCY L 摘要:The present invention provides methotrexate analogs having the formula: +TR wherein R is methyl or hydro, X is halo or hydro, and D1 is -NR1R2 wherein either both R1 and R2 are hydrogen, or one is hydrogen and the other is C1-C5 alkyl, C1-C5 haloalkyl, cyano C1-C5 alkyl, C1-C5 hydroxyalkyl, alkoxyalkyl wherein the alkoxy and the alkyl have 1-5 carbon atoms, carboxy C1-C5 alkyl, phenyl, C1-C5 alkyl phenyl, C(=O)R' wherein R' is hydrogen, C1-C5 alkyl, phenyl, or C1-C5 alkyl phenyl, C(=O)OR'' wherein R'' is hydrogen, C1-C5 alkyl, phenyl, or C1-C5 alkyl phenyl, amino, C(=NH)NH2, C(=O)NH2, or C(=S)NH2, and structurally related derivatives, as well as pharmaceutical compositions comprising such MTX analogs, methods of synthesis of the MTX analogs, and use of the MTX analogs in modulating cellular functions, or in treating cancer and other diseases or disorders capable of being treated using MTX.
专利号:US-5382582-A 优先权日:1993-03-26 标题:Methotrexate analogs and methods of using same 发明人:CHAN CARCY L 摘要:The methotrexate analogs 7-d-MTX, 7,9,9-d3-MTX, MTX halogenated or possessing some other such group at the 7-position capable of reducing oxidation to 7-OH-MTX, and structurally related analogs, as well as pharmaceutical compositions containing the analogs, the synthesis of the MTX analogs, and use of the analogs in modulating cellular function.
专利号:US-5981748-A 优先权日:1995-06-07 标题:Synthesis of optically pure compounds useful as GARFT inhibitors and their intermediates 发明人:VARNEY MICHAEL D; ROMINES WILLIAM H; PALMER CYNTHIA L 权利人:AGOURON PHARMA 摘要:The invention relates to methods of making compounds of the formula VII ##STR1## and their enantiomers, where Ar is a substituted or unsubstituted five- or six-membered aromatic group and B is either an amino acid linked through the amino portion to form an amide or a C 1 -C 6 alcohol linked through the alcohol portion to form an ester. These compounds are advantageously employed as intermediates to prepare optically pure compounds that are active GARFT inhibitors. In one method, a compound of the formula ##STR2## is reacted with a compound of the formula ##STR3## where X is a halogen.
摘要:S13 | EUCOSMETICS | Combined Inventory of Ingredients Employed in Cosmetic Products (2000) and Revised Inventory (2006) | DOI:10.5281/zenodo.2624118 参考文献:10.1021/jm010575m 摘要:Gangjee A, Zeng Y, McGuire JJ, Kisliuk RL. Synthesis of N-[4-[1-Ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic Acid as an Antifolate. J. Med. Chem. 2002 Mar 21;45(9):1942–8. doi: 10.1021/jm010575m. 参考文献:10.1002/jnr.490150309 摘要:Salazar P, Quesada O, Campomanes MA, Morán J, Pasantes‐Morales H. Pharmacological identification of retinal cells releasing taurine by light stimulation. J of Neuroscience Research. 1986 Jan;15(3):383–91. doi: 10.1002/jnr.490150309. 参考文献:10.1007/bf00971574 摘要:Kabuto H, Yokoi I, MoonSuk S, Yamamoto M, Mori A. Effects of kainic acid, quisqualic acid, and their antagonist, pCB-PzDA, on rat electrocorticograms and monoamine metabolite levels in rat striatum. Neurochem Res. 1994 Mar;19(3):267–74. doi: 10.1007/bf00971574. 参考文献:10.1016/0361-9230(94)90236-4 摘要:Peeters BW, Ramakers GM, Vossen JM, Coenen AM. The WAG/Rij rat model for nonconvulsive absence epilepsy: involvement of nonNMDA receptors. Brain Res Bull. 1994;33(6):709–13. doi: 10.1016/0361-9230(94)90236-4.