5382-16-1Relevant articles and documents
PRODUCTION METHOD OF CYCLIC COMPOUND
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Paragraph 0057; 0059; 0062-0064, (2021/05/05)
PROBLEM TO BE SOLVED: To provide an industrially simple production method of a cyclic compound. SOLUTION: A production method of a cyclic compound includes a step to obtain a reduced form (B) by reducing an unsaturated bond in a ring structure of an aromatic compound (A) by means of catalytic hydrogenation of the aromatic compound (A) or its salt using palladium carbon as a catalyst under a normal pressure, in which the aromatic compound (A) has one or more ring structures selected from a group consisting of a five membered-ring, a six membered-ring, and a condensed ring of the five membered-ring or the six membered-ring with another six membered-ring, a hetero atom can be included in the ring structure, and the aromatic compound (A) can have one or two side chains bonded to the ring structure and does not have any carbon-carbon triple bond in the side chain. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
Method for regulating and controlling catalytic hydrogenation reaction of pyridine derivative with redox potential
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Paragraph 0036-0043, (2019/05/08)
The invention discloses a method for regulating and controlling catalytic hydrogenation reactions of a pyridine derivative with redox potential. On the basis of data such as redox potential (ORP) andcatalytic hydrogenation reaction process of the pyridine derivative in different medium systems, a scheme that the catalytic hydrogenation reaction of the pyridine derivative is promoted by improvingpyridine derivative ORP with an acid water solution is proposed. As the catalytic hydrogenation reactions of the pyridine derivative are instructed with ORP data, the testing period is shortened, meanwhile, by adopting the process, the pressure of hydrogenation reactions can be reduced, a piperidine product has the advantages of being high in purity, convenient in aftertreatment, and the like, andthus great instruction significances can be achieved for industrial development of the pyridine derivative.
Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: Effects of the phenyl substituent and the linker orientation
Zeng, Li-Fan,Jiang, Xiao-Hua,Sanchez, Tino,Zhang, Hu-Shan,Dayam, Raveendra,Neamati, Nouri,Long, Ya-Qiu
, p. 7777 - 7787 (2008/12/23)
Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity relationship (SAR) study with respect to the substituent effect of the ADK and the dimerization with conformationally constrained linkers such as piperazine, 4-amino-piperidine, piperidin-4-ol, and trans-cyclohexan-1,4-diamine. The substituents on the phenyl ring as well as the spatial orientation of the two diketo units were observed to play important roles in the IN inhibitory potency. The hydrophobic group was an optimal substitution at the 3-position of the aryl ring. The piperazine and 4-amino-piperidine linkers brought about the most potent analogs among the hydrophobic group or halogen substituted ADK dimers. The docking studies suggested that the bulky hydrophobic substitution at 3-phenyl ring and the linker of 4-amino-piperidine were beneficial for adopting an active conformation to achieve strong interactions with the active site Mg2+ and the key residue E152 within the catalytic core domain. This study is a significant extension of our previous report on the dimeric ADK-containing IN inhibitors, providing a new promising template for further lead optimization.