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-8828984-B2 优先权日:2012-11-19 标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection 发明人:CHE CHI MING; ZOU TAOTAO 权利人:UNIV HONG KONG; UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.
专利号:US-10577387-B1 优先权日:2018-08-09 标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment 发明人:CHE CHI MING; Fung Sin Ki; Chen tian feng 权利人:UNIV HONG KONG 摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
专利号:US-11286271-B2 优先权日:2018-07-31 标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment 发明人:CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG 权利人:UNIV HONG KONG 摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
专利号:WO-2016122420-A1 优先权日:2015-01-26 标 题 :An improved method for the synthesis and purification of pirfenidone 发明人:KOYUNCU HASAN; AKGOL EMRE; REIS OMER 权利人:ULKAR KIMYA SANAYII VE TICARET A S 摘要:The present invention provides a process for the synthesis of pirferidone by reacting 5-methyl-2-pyridone with a low quantity of bromobenzene in a low quantity of polar aprotic solvent in the presence of a copper catalyst and a base. The present invention also provides a method for purification of pirfenidone by initially synthesizing an acid adduct of pirfenidone from crude pirfenidone and then recovering pirfenidone with increased purity.
1: Kang J, Lee KH, Lee JH, Jeong YY, Choi SM, Kim HC, Park JH, Lee HK, Yong SJ, Choi HS, Kim HR, Jegal Y, Choi WI, Lee EJ, Song JW. Safety, effectiveness, and usefulness of higher-dose tablets of generic pirfenidone in patients with IPF: a nationwide observational study in South Korea. Front Pharmacol. 2024 Aug 9;15:1451447. doi: 10.3389/fphar.2024.1451447. 2: Bai Y, Liu F, Luo S, Wan Y, Zhang L, Wu X, Chen Q, Xie Y, Guo P. Experimental study on H2O2 activation of HSC-T6 and hepatic fibrosis in cholestatic mice by "Yajieshaba". J Ethnopharmacol. 2024 Aug 22;335:118712. doi: 10.1016/j.jep.2024.118712. Epub ahead of print. 11:1411279. doi: 10.3389/fmed.2024.1411279.
合成参考文献
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