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4,4-二甲基-2,6-二氧代哌啶-3,5-二甲腈置于硫酸,水,乙酸酐体系中,化学反应 18.0H,反应生成 3,3-二甲基戊二酸酐
参考文献:The Development Of A New Class Of Inhibitors For Betaine-Homocysteine S-Methyltransferase
标题:The Development Of A New Class Of Inhibitors For Betaine-Homocysteine S-Methyltransferase
摘要:Betaine-Homocysteine S-Methyltransferase (Bhmt) Is An Important Zinc-Dependent Methyltransferase That Uses Betaine As The Methyl Donor For The Remethylation Of Homocysteine To Form Methionine. In The Liver,Bhmt Performs To Half Of The Homocysteine Remethylation. In This Study,We Systematically Investigated The Tolerance Of The Enzyme For Modifications At The "Homocysteine" Part Of The Previously Reported Potent Inhibitor (R,S)-5-(3-Amino-3-Carboxy-Propylsulfanyl)-Pentanoic Acid (1). In The New Compounds,Which Are S-Alkylated Homocysteine Derivatives,We Replaced The Carboxylic Group In The "Homocysteine" Part Of Inhibitor 1 With Different Isosteric Moieties (Tetrazole And Oxadiazolone); We Suppressed The Carboxylic Negative Charge By Amidations; We Enhanced Acidity By Replacing The Carboxylate With Phosphonic Or Phosphinic Acids; And We Introduced Pyrrolidine Steric Constraints. Some Of These Compounds Display High Affinity Toward Human Bhmt And May Be Useful For Further Pharmacological Studies Of This Enzyme. Although None Of The New Compounds Were More Potent Inhibitors Than The Reference Inhibitor 1,This Study Helped To Completely Define The Structural Requirements Of The Active Site Of Bhmt And Revealed The Remarkable Selectivity Of The Enzyme For Homocysteine. (C) 2013 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2013.04.039

专利信息

专利号:US-2022098170-A1
优先权日:2019-01-16
标 题 :Process for the synthesis of gepirone
发明人：COLOMBANO GIAMPIERO; BARBERO MAURO; GIOVENZANA GIOVANNI BATTISTA; ROLETTO JACOPO; PAISSONI PAOLO
权利人:PROCOS SPA
摘要:Disclosed is a process for the synthesis of gepirone of formula (I) from 8-(pyrimidin-2-yl)-5,8-diazaspiro[4,5]decan-5-ium bromide. The process according to the invention is economically efficient and easily industrially scalable.

专利号:US-2023357257-A1
优先权日:2020-12-28
标 题 :Novel process for the synthesis of noroxymorphone from morphine
发明人：GORBACHEV DMITRY; LAM HON WAI; SAXENA AAKARSH; SAXENA NAVIN SATYAPAL
权利人:NAVIN SAXENA RESEARCH & TECH PVT LTD
摘要:The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents and solvents of lesser toxicity and lower cost with respect to those used in the prior art.

专利号:US-5726344-A
优先权日:1994-07-13
标题 :Enantiomeric enrichment of bicyclic alcohols
发明人：WEST J BLAIR; DEVRIES Keith
权利人:BEND RES INC
摘要:There is disclosed a two-stage enzymatically catalyzed reaction for the selective preparation of the (R)-endo-isomer of norbornenol from a mixture containing all four stereo- and regioisomers of norbornenol, as well as the synthesis of the intermediate product comprising the enantiomerically enriched mono-ester of (R)-endo-norbornenol and a diacid, and of the enantiomerically enriched saturated alcohol (R)-endo-norborneol. There is also disclosed a method for the production of (R)-endo-norborne-2-ol, by chemical reduction of either the enantiomerically enriched monoester and subsequent hydrolysis, or by hydrolysis of the enantiomerically enriched monoester and then chemical reduction.

专利号:WO-2025124564-A1
优先权日:2023-12-15
标题:Polyester synthesis based on aspartic acid modification
发明人：ZHANG KECHUN; CHEN XI; LEI TENGFEI; LIU SHENGYANG
权利人:MINT BIOTECHNOLOGIES CO LTD
摘要:Provided in the present invention is polyester synthesis based on aspartic acid modification. A monomer of a unique structure of an imide ring is obtained based on aspartic acid and a dibasic acid likely to be cyclized, the monomer is based on the aspartic acid, can be derived from biomass, is low in cost and renewable, meets the requirement of sustainable development, and the unique structure of the monomer can regulate and control various properties of polyester materials, such as the mechanics, temperature resistance, hydrophilicity and hydrophobicity, and crystallization.

专利号:EP-0658564-B1
优先权日:1986-04-30
标题 :Electroluminescent compounds and intermediates in their synthesis
发明人：MASSEY RICHARD J; POWELL MICHAEL J; MIED PAUL A; POONIAN MOHINDAR S; FENG PETER; CIANA LEOPOLDO DELLA; DRESSICK WALTER J
权利人:IGEN INT INC
摘要:Novel compounds for use in electrochemiluminescent assays and characterised by containing the structure        X - Y - ZwhereinX represents one or more nucleotides which may be the same or different, one or more amino acids which may be the same or different, an antibody, an analyte of interest or an analogue of an analyte of interestY represents a linker group attached to X and Z,andZ represents an electrochemiluminescent moiety, and intermediates employed in their synthesis.

专利号:US-6326372-B1
优先权日:1999-09-30
标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
发明人：EVANS BEN E; GILBERT KEVIN F
权利人:MERCK & CO INC
摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.