30557-06-3Relevant academic research and scientific papers
Room Temperature Benzofused Lactam Synthesis Enabled by Cobalt(III)-Catalyzed C(sp2)?H Amidation
Tian, Xun,Li, Xin,Duan, Shengzu,Du, Ya,Liu, Tongqi,Fang, Yongsheng,Chen, Wen,Zhang, Hongbin,Li, Minyan,Yang, Xiaodong
, p. 1050 - 1058 (2020/12/18)
Benzofused lactams, especially indolin-2-one and dihydroquinolin-2-one are popular structural motives in durgs and natural products. Herein, we developed a room temperature and robust synthesis of benzofused lactams through cobalt(III)-catalyzed C(sp
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3
Bromidge, Steven M.,Arban, Roberto,Bertani, Barbara,Borriello, Manuela,Capelli, Anna-Maria,Di-Fabio, Romano,Faedo, Stefania,Gianotti, Massimo,Gordon, Laurie J.,Granci, Enrica,Pasquarello, Alessandra,Spada, Simone K.,Worby, Angela,Zonzini, Laura,Zucchelli, Valeria
supporting information; experimental part, p. 7092 - 7096 (2011/01/03)
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT1 autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The
PYRIMIDINE COMPOUNDS AND USE THEREOF
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Page/Page column 45, (2010/02/15)
The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C=W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N-Rk or a group CRmRn; D represents C=O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N-Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2-CH2 or CH2-CH2-CH2; M represents CH or N; Y represents CH2, CH2-CH2 or CH2-CH2-CH2 or M-X, together, represent CH=C or CH2-CH=C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rk, Rp, R1, R2, R3, R4, R5 and R6 have the meanings cited in the claims and in the description. The invention also relates to the physiologically compatible acid addition salts of the aforementioned compounds, and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
A study on the conversion of indanones into carbostyrils
Torisawa, Yasuhiro,Nishi, Takao,Minamikawa, Jun-Ichi
, p. 2205 - 2209 (2007/10/03)
We have surveyed the utility of Beckmann rearrangement for the conversion of indanones into carbostyrils. Initial attempts at the conversion of 6-methoxy indanone oxime under classical conditions resulted in the formation of the two unusual products: 2-sulfonyloxyindanone and the dimeric product. This unusual rearrangement was also observed by the treatment of some metal triflates species. Further investigation has led to the development of reliable conditions starting from oxime mesylate (not oxime tosylate), in which some strong Lewis acid catalyst (ZrCl4) was employed in either a conventional or non-conventional solvent system. The advantage of the new protocol is highlighted by the simple work up and direct isolation of the product in 65% isolated yield.
Synthetic Application of Lithiation Reactions: A Convenient Synthesis of 3,4-Dihydro-5-hydroxycarbostyril, 1,2,3,4-Tetrahydro-5-hydroxy-2-oxo-1,7-naphthyridine, and Methyl 3-Methoxypyridine-4-carboxylate
Tamura, Yasumitsu,Chen, Ling Ching,Fujita, Masanobu,Kita, Yasuyuki
, p. 1257 - 1262 (2007/10/02)
3,4-Dihydro-5-hydroxycarbostyril (3), a key intermediate for a clinically used β-receptor blocking agent (1), and its 7-aza analog (4) were prepared by an acid-catalyzed cyclization of the N-pivaloylamino-esters (17 and 19), which were obtained by using o
