碘甲烷置于1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 二氯甲烷 用作溶剂,化学反应 20.0H,以82%的收率获得5-溴-2-糠酸甲酯 参考文献: Heterocyclic Silicon Compounds And Their Use In The Treatment Of Diseases Or Conditions Associated With Gnrh (Gonadotropin-Releasing Hormone)[fr] Composes De Silicium Heterocycliques Et Utilisation De Ceux-Ci Dans Le Traitement De Maladies Ou D'Etats Associes A Gnrh (Hormone De Liberation De La Gonadotropine) 标题: Heterocyclic Silicon Compounds And Their Use In The Treatment Of Diseases Or Conditions Associated With Gnrh (Gonadotropin-Releasing Hormone)[fr] Composes De Silicium Heterocycliques Et Utilisation De Ceux-Ci Dans Le Traitement De Maladies Ou D'Etats Associes A Gnrh (Hormone De Liberation De La Gonadotropine) 摘要:式(i)的化合物,其中x和y中的一个是硅,另一个是碳或硅;Z是氧,硫或-N(R)-,其中r是氢或烷基;R1是氢,卤素,烷基,烯基,炔基,烷氧基或环烷基;R2是烷基,烯基,炔基,环烷基,杂环烷基,芳基,杂芳基,-烷基-环烷基,-烷基-杂环烷基,-烷基-芳基或-烷基-杂芳基;或其药学上可接受的盐.这些化合物用于制造治疗或预防与gnrh(促性腺激素释放激素)相关的疾病或症状的药物,例如用于治疗或预防癌症(例如白血病治疗),生育障碍,Hiv感染或艾滋病,阿尔茨海默病,纤维化,子宫内膜异位症,子宫肌瘤或子宫平滑肌瘤的进展.
专利号:US-2020181095-A1 优先权日:2017-06-06 标题:Selective matrix metalloproteinase-13 inhibitors 发明人:FIELDS GREGG B; ROUSH WILLIAM R; CHOI JUN YONG; FUERST RITA 权利人:FLORIDA ATLANTIC UNIV BOARD OF TRUSTEES; SCRIPPS RESEARCH INST 摘要:We describe the use of comparative structural analysis and structure-guided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metalloproteinase 13 (MMP-13). We applied a three-step process, starting with a comparative analysis of the X-ray crystallographic structure of compound 5 in complex with MMP-13 with published structures of known MMP-13 inhibitor complexes followed by molecular design and synthesis of potent, but non-selective zinc-chelating MMP inhibitors (e.g., 10a and 10b). After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-10a, and 10b were binding within the MMP-13 active site, the Zn2+ chelating unit was replaced with non-chelating polar residues that bridged over the Zn2+ binding site and reach into a solvent accessible area. After two rounds of structural optimization, these design approaches led to small molecule MMP-13 inhibitors 10d and (S)-17b which bind within the substrate-binding site of MMP-13 and surround the catalytically active Zn2+ ion without chelating to the metal. These compounds exhibit at least 500-fold selectivity versus other MMPs.
专利号:US-2022048879-A1 优先权日:2020-08-13 标 题:Synthesis of small molecules inspired by Phomoxanthone A 发明人:ALI RAMEEZ; MATTSON ANITA 权利人:WORCESTER POLYTECH INST 摘要:Methods, compositions, and kits are provided for synthesizing bioactive chromane, the method including: constructing a tertiary ether stereocenter enantioselectively by catalyzed alkynylation of a substituted chromenone to obtain a chromanone; reducing alkyne and ketone in the chromanone to obtain a chroman; and converting ester to methyl group thereby obtaining chromane.
专利号:US-2024335420-A1 优先权日:2021-08-02 标题:N-acylhydrazone compounds capable of inhibiting nav 1.7 and/or nav 1.8, processes for the preparation thereof, compositions, uses, methods for treatment using same and kits 发明人:BARREIRO GABRIELA; SANT'ANA DANILO PEREIRA DE; GAMBA LUIS EDUARDO REINA; FRAGA CARLOS ALBERTO MANSSOUR; BARREIRO ELIEZER JESUS DE LACERDA; LIMA LÃ?DIA MOREIRA 权利人:EUROFARMA LABORATORIOS S A; UNIV FEDERAL DO RIO DE JANEIRO UFRJ 摘要:N-Acylhydrazone compounds that are Nav 1.7 and/or Nav 1.8 inhibitors, including N-acylhydrazone compounds of Formula (I), wherein substituents R1 to R4 are independently selected from the groups defined in the specification, as well as to the processes for the preparation thereof, compositions comprising at least one of these compounds, uses, treatment methods for treating or preventing pain-related pathologies, and kits, useful in the fields of medicinal chemistry, organic synthesis, as well as in the treatment of pain-related disorders.
专利号:US-9751877-B2 优先权日:2012-09-21 标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:WO-2022069554-A1 优先权日:2020-10-01 标 题:Method for producing 4-bromfuran-2-carboxylates 发明人:REMBIAK ANDREAS 权利人:BAYER AG 摘要:The invention relates to a method for producing 4-bromofuran-2-carboxylates of general formula (I) and to the use thereof as important precursors for the synthesis of agrochemical and pharmaceutical active substances. (I).
专利号:WO-2005082899-A1 优先权日:2004-01-28 标 题:Oxazolidinone derivatives as antimicrobials 发明人:SALMAN MOHAMMAD; BISWAJIT DAS; RUDRA SONALI; YADAV AJAY SINGH; RATTAN ASHOK 权利人:RANBAXY LAB LTD; SALMAN MOHAMMAD; BISWAJIT DAS; RUDRA SONALI; YADAV AJAY SINGH; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones of formula (I) and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing such compounds as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
参考标题:Synthesis Of Amido-N-Imidazolium Salts And Their Applications As Ligands In Suzuki-Miyaura Reactions: Coupling Of Hetero- Aromatic Halides And The Synthesis Of Milrinone And Irbesartan 作者:Manian Rajesh Kumar,Kyungho Park,Sunwoo Lee |发布日期:2010.12.17 摘要:Catalytic System Based On Palladium-Amido-N-Heterocyclic Carbenes For Suzuki-Miyaura Coupling Reactions Of Heteroaryl Bromides Is Described. A Variety Of Sterically Bulky, Amido-N-Imidazolium Salts Were Synthesized In High Yields From The Corresponding Anilines. This Catalytic System Effectively Promoted Suzuki-Miyaura Couplings Of Heteroaryl Bromides And Chlorides With A Range Of Boronic Acids To
合成参考文献
摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 357. 摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 261. 摘要:Andersson, C.-M.; Andersson, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 42. 摘要:Shi, L., Science of Synthesis: Knowledge Updates, (2024) 1, 10.