专利号:US-12331021-B2 优先权日:2020-09-10 标题 :Total synthesis of pirfenidone 发明人:ZHOU LIHUA 权利人:SUZHOU FUDE ZHAOFENG BIOCHEMICAL TECH CO LTD 摘要:The present invention relates to a process for the synthesis of Pirfenidone (1) from 5-Methyl-3,4-dihydro-2-pyridone and halobenzene (chlorobenzene, bromobenzene, or iodobenzene) in the presence of a catalytic system consisting of a copper salt and an organic ligand, in the presence of a base.
专利号:US-10472325-B2 优先权日:2015-10-29 标题:Process for the synthesis of pirfenidone 发明人:MOSSOTTI MATTEO; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of Pirfenidone (1) from 5-methyl-2(1H)-pyridinone and chlorobenzene in the presence of a catalytic system consisting of a copper salt and an organic ligand, in the presence of a base. n n n n n n n n n n The process exploits the high efficiency of the catalytic system consisting of copper(I) salt and an organic ligand in the presence of an inorganic base in the N-amidation reaction of chlorobenzene, a cheap reagent also usable as solvent in this case; reaction conditions at high temperatures, at atmosphere pressure or higher, produce a reaction with good yields.
专利号:US-4557866-A 优先权日:1984-05-15 标 题 :Process for the synthesis of pyrido-imidazo rifamycins 发明人:CANNATA VINCENZO; TAMAGNONE GIAN F 权利人:ALFA FARMACEUTICI SPA 摘要:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1-4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin O of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before.
专利号:US-2023303611-A1 优先权日:2022-01-21 标题:Synthesis of an antiviral azasugar triphosphate 发明人:KOTIAN PRAVIN L; Dang zhao; WU MINWAN 权利人:BIOCRYST PHARM INC 摘要:Provided are methods of making the active 5′-triphosphate form of galidesivir (compound 1) and the active 5′-triphosphate form of azasugar nucleoside analogues (compound 2):a potent anti-viral compound useful for broad spectrum treatment, suppression, and prevention of viral infections. The syntheses of compound 1 and compound 2 can be achieved via selective formation of protected intermediate 1b and protected intermediate 2b, respectively:
专利号:US-2005054669-A1 优先权日:2003-07-31 标 题 :Process for the synthesis of zolpidem 发明人:KUMAR YATENDRA; PRASAD MOHAN; NATH ASOK 摘要:The present invention relates to processes for the preparation of zolpidem of Formula V as shown in the accompanying drawings or pharmaceutically acceptable salts thereof from N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula II. The process includes (a) reacting N,N-dimethyl-3-(4-methyl)benzoyl propionamide of Formula II with bromine to get the bromo amide of Formula III; (b) condensing the bromo amide of Formula III with 2-amino-5-methylpyridine of Formula IV to get the zolpidem base of Formula V; and (c) converting zolpidem base of Formula V to its hemitartarate salt of Formula VII.
专利号:US-RE42890-E 优先权日:2003-05-23 标题 :Furazanobenzimidazoles 发明人:EBERLE MARTIN; BACHMANN FELIX; STREBEL ALESSANDRO; ROY SUBHO; SRIVASTAVA SUDHIR; SAHA GOUTAM 权利人:BASILEA PHARMACEUTICA AG 摘要:The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R 1 to R 6 have the meanings given in the specification, for use as medicaments, to novel compounds of formula (I), to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same
摘要:Ayaz, M.; De Moliner, F.; Morales, G. A.; Hulme, C., Science of Synthesis: Multicomponent Reactions, (2013) 1, 116. 摘要:Wessjohann, L. A.; Kaluđerović, G. N.; Neves Filho, R. A. W.; Morejon, M. C.; Lemanski, G.; Ziegler, T., Science of Synthesis: Multicomponent Reactions, (2013) 1, 432. 摘要:Prehled Prumyslove Toxikologie; Organicke Latky, Marhold, J., Prague, Czechoslovakia, Avicenum, 1986, -(841), 1986 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. 摘要:P.J. Brignell, C.D. Johnson, A.R. Katritzky, N. Shakir, H.O. Tarhan and G. Walker. J. Chem. Soc., B 1967, 1233.