环戊酮置于barium Dihydroxide,Sodium Hydroxide,碳酸氢铵体系中,用 乙醇,水,叔丁醇 作为反应溶剂,化学反应 13.0H,反应生成 Boc-1-氨基环戊烷羧酸 参考文献:Synthesis And Structure-activity Relationships Of Potential Anticonvulsants Based On 2-Piperidinecarboxylic Acid And Related Pharmacophores 标题:Synthesis And Structure-activity Relationships Of Potential Anticonvulsants Based On 2-Piperidinecarboxylic Acid And Related Pharmacophores 摘要:Using N-(2,6-Dimethyl)Phenyl-2-Piperidinecarboxamide (1) And N-(Alpha-Methylbenzyl)-2-Piperidinecarboxamide (2) As Structural Leads,A Variety Of Analogues Were Synthesised And Evaluated For Anticonvulsant Activity In The Mes Test In Mice. In The N-Benzyl Series,Introduction Of 3-Cl,4-Cl,3,4-Cl-2,Or 3-Cf3 Groups On The Aromatic Ring Led To An Increase In Mes Activity. Replacement Of The Alpha-Methyl Group By Either I-Pr Or Benzyl Groups Enhanced Mes Activity With No Increase In Neurotoxicity. Substitution On The Piperidine Ring Nitrogen Led To A Decrease In Mes Activity And Neurotoxicity,While Reduction Of The Amide Carbonyl Led To A Complete Loss Of Activity. Movement Of The Carboxamide Group To Either The 3-Or 4-Positions Of The Piperidine Ring Decreased Mes Activity And Neurotoxicity. Incorporation Of The Piperidine Ring Into A Tetrahydroisoquinoline Or Diazahydrinone Nucleus Led To Increased Neurotoxicity. In The N-(2,6-Dimethyl)Phenyl Series,Opening Of The Piperidine Ring Between The 1-And 6-Positions Gave The Active Norleucine Derivative 75 (Ed50 = 5.8 Mg Kg(-1),Td50 = 36.4 Mg Kg(-1),Pi = 6.3). Replacement Of The Piperidine Ring Of I By Cycloalkane (Cyclohexane,Cyclopentane,And Cyclobutane) Resulted In Compounds With Decreased Mes Activity And Neurotoxicity,Whereas Replacement Of The Piperidine Ring By A 4-Pyridyl Group Led To A Retention Of Mes Activity With A Comparable Pi. Simplification Of The 2-Piperidinecarboxamide Nucleus Of 1 Into A Glycinecarboxamide Nucleus Led To About A Six-Fold Decrease In Mes Activity. The 2,6-Dimethylanilides Were The Most Potent Compounds In The Mes Test In Each Group Of Compounds Evaluated,And Compounds 50 And 75 Should Be Useful Leads In The Development Of Agents For The Treatment Of Tonic-Clonic And Partial Seizures In Man. (C) 2001 Editions Scientifiques Et Medicales Elsevier Sas. DOI:10.1016/s0223-5234(00)01206-X
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-7741492-B2 优先权日:2005-02-28 标题:Method for obtaining a pharmaceutically active compound (Irbesartan) and its synthesis intermediate 发明人:HUGUET CLOTET JOAN; DALMASES BARJOAN PERE 权利人:INKE SA 摘要:It is provided a method for obtaining Irbesartan polymorph A, with few synthesis steps, by coupling the intermediate of formula (II) with the compound of formula (III), neutralising one of its alkaline salts in an aqueous medium and recrystallising the crude product obtained. The utilisation of said method obviates protection and deprotection of the tetrazole ring and is therefore of considerable interest for obtaining Irbesartan on a large industrial scale. The invention also refers to the synthesis intermediate of formula (II).
专利号:US-5175146-A 优先权日:1989-12-05 标题 :Synthetic calcitonin peptides 发明人:BASAVA CHANNA; HOSTETLER KARL Y 权利人:VICAL INC 摘要:Synthetic hypocalcemic peptides which are similar in biological properties to native calcitonins as clinically useful agents. The peptides comprise analogues of native calcitonins having amino acid substitutions and deletions which act to improve potency, prolong duration of the hormonal effect, enhance receptor binding, and increase oral or nasal bioavailability. The calcitonin peptide analogues are less expensive and more easily synthesized than native calcitonins, and have improved resistance to inactivation or degradation. Methods are provided for the synthesis of these peptides. Also, disclosed are novel cyclic peptides, including calcitonin, having increased stability with respect to proteolysis. Methods for the synthesis of these peptides are provided, comprising converting disulfide cyclic peptides and proteins to enzymatically and chemically stable cyclic peptide structures by the replacement of cysteine residues with dicarboxylic acids and diamino acids. The method is applicable to various naturally occurring peptides, their synthetic analogues or derivatives, and proteins.
专利号:ES-2291099-A1 优先权日:2005-02-28 标题 :IMPROVEMENTS IN THE OBJECT OF THE MAIN PATENT NUM. 200500485, BY 'PROCEDURE FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND AND ITS SYNTHESIS INTERMEDIATE'.
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合成参考文献
参考文献:10.1007/s11426-023-1812-x 摘要:Li S, Jiang Y, Luo X, Ran X, Li Y, Wu D, Pan C, Xia P. Photocatalytic vinyl radical-mediated multicomponent 1,4-/1,8-carboimination across alkynes and olefins/(hetero)arenes. Sci. China Chem. 2023 Sep 27;67(2):558–67. doi: 10.1007/s11426-023-1812-x. 参考文献:10.1038/nchembio.132 摘要:Van Zeebroeck G, Bonini BM, Versele M, Thevelein JM. Transport and signaling via the amino acid binding site of the yeast Gap1 amino acid transceptor. Nat Chem Biol. 2009 Jan;5(1):45–52. doi: 10.1038/nchembio.132.