丙二酸二甲酯 在 Potassium Hydroxide体系中,用 甲醇作为反应溶剂,以71%的收率获得monomethyl Monopotassium Malonate 参考文献:Formation And Loading Of A (2S)‐2‐ethylmalonamyl Starter Unit In The Assembly Line Of Polyketide‐nonribosomal Peptide Hybrid Sanglifehrin A 标题:Formation And Loading Of A (2S)‐2‐ethylmalonamyl Starter Unit In The Assembly Line Of Polyketide‐nonribosomal Peptide Hybrid Sanglifehrin A 摘要:摘要长寿素 A(Sfa)是一种螺内酰胺共轭的 22 元大环内酯,具有显著的免疫抑制和抗病毒活性.这种大环内酯是多酮肽合成酶(Pks)-非核糖体肽合成酶(Nrps)混合装配线的产物,利用 (2S)-2-乙基丙二酰基作为起始单元.在这里,我们报告了这种起始单元在 Sfa 组装线中的形成和装载涉及两个不同寻常的酶促反应,它们发生在一个离散的酰基载体蛋白(Acp)Sfao 上.酰胺合成酶 Sfap 以依赖 Sfao 的方式催化 (2S)-2-Ethylmalonyl 的酰胺化反应.然后,β-酮酰-Acp 合酶 Iii 样蛋白 Sfan 将 Sfao 产生的 (2S)-2-Ethylmalonamyl 转移到混合 Pks-Nrps 组装线的负载 Acp 结构域上,为 Sfa 的生物合成提供能量.Sfap 和 Sfan 都具有杂交活性.这项研究为不寻常结构单元的形成和结合提供了一个新的范例,从而进一步加深了对组装线化学的认识. Doi:10.1002/Anie.202217090
专利号:WO-2024260325-A1 优先权日:2023-06-19 标题 :Synthesis of macrocyclic compound and medical use of macrocyclic compound 发明人:LU HONGFU; DING XIAO; REN FENG 权利人:INSILICO MEDICINE IP LTD 摘要:Provided in the present invention are the synthesis of a macrocyclic compound and the medical use of the macrocyclic compound. Specifically, provided in the present invention are a compound as show in formula (II), a stereoisomer thereof or a pharmaceutically acceptable salt thereof, which can be used as a CDK7 inhibitor.
专利号:US-5124478-A 优先权日:1987-12-22 标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method 发明人:BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER 权利人:HOECHST AG 摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.
专利号:US-9932361-B2 优先权日:2013-02-20 标题:Convenient process for the preparation of statins 发明人:DE LUCCHI OTTORINO; TARTAGGIA STEFANO; FERRARI CLARK; GALVAGNI MARCO; PONTINI MARTA; FOGAL STEFANO; MOTTERLE RICCARDO; MORENO ROSA MARIA; COMELY ALEX 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
专利号:PT-89297-B 优先权日:1987-12-22 标题 :METHOD FOR PREPARING NEW INTERMEDIATE COMPOUNDS FOR PEPTIDE SYNTHESIS AND PROCESS FOR SYNTHESIS OF PEPTIDE-AMIDES BY THE SOLID PHASE METHOD USING THE REFERRED COMPOUNDS
专利号:US-5837877-A 优先权日:1996-02-02 标题 :Process for preparing optically active 4-hydroxy-2-pyrrolidone 发明人:MITSUHASHI SHIGERU; KUMOBAYASHI HIDENORI 权利人:TAKASAGO PERFUMERY CO LTD 摘要:A process for preparing optically active 4-hydroxy-2-pyrrolidone comprising asymmetrically hydrogenating an N-substituted-4-amino-3-oxobutanoic ester represented by formula (I): ##STR1## wherein R 1 represents a benzyloxycarbonyl group, the benzene ring of which may be substituted; and R 2 represents a lower alkyl group having 1 to 4 carbon atoms, in the presence of a ruthenium-optically active phosphine complex as a catalyst to obtain an optically active N-substituted-4-amino-3-hydroxybutanoic ester, deblocking, and cyclizing the ester. A series of the reactions can be carried out in one pot. Optically active 4-hydroxy-2-pyrrolidone is obtained in high yield with high optical purity, and is useful in the synthesis of carbapenem antibiotics
专利号:US-2012172350-A1 优先权日:2009-09-11 标题 :Histamine h3 inverse agonists and antagonists and methods of use thereof 发明人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN 权利人:CHYTIL MILAN; ENGEL SHARON R; FANG QUN KEVIN; SUNOVION PHARMACEUTICALS INC 摘要:Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.