161233-97-2Relevant articles and documents
Method for converting halogenopyridinecarboxylic acid into cyanopyridinecarboxylic acid
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Paragraph 0047-0050, (2019/07/04)
The invention provides a method for converting halogenopyridinecarboxylic acid into cyanopyridinecarboxylic acid. The method is characterized in that the halogenopyridinecarboxylic acid reacts with acyanidation reagent to form the cyanopyridinecarboxylic acid. The preparation method makes the halogenopyridinecarboxylic acid directly converted into the cyanopyridinecarboxylic acid in one step, sothe method has the advantages of omission of esterification and hydrolysis steps, simplification of synthesis steps, shortening of the reaction process, manpower saving, productivity increase, reduction of three wastes, suitableness for industrial production, and broad application prospect.
A 2 - cyano-isonicotinic acid hydrazide 1.5 paratoluene sulfonate synthetic method (by machine translation)
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Paragraph 0012; 0013; 0015, (2017/08/26)
A 2-cyano isonicotinic acid hydrazide 1.5 p-toluenesulfonate synthetic method is as follows: 2-cyano methyl isonicotinate is used as a starting material for alkali hydrolysis to obtain 2-cyano isonicotinic acid, the 2-cyano isonicotinic acid is condensed with tertiary butoxy carbonyl hydrazine under the action of a condensing agent, and the condensation compound is hydrolyzed with p-toluenesulfonate monohydrate to obtain a target compound. The process does not need high temperature or low temperature reaction, and does not need an inert gas for protection, all reaction solvents do not need non-water pretreatment, an intermediate does not need purification, reaction condition is mild, operation is simple, and the method is suitable for industrial production.
COMPOUNDS AND METHODS for the inhibition of HDAC
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, (2015/11/24)
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3, 14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido] morphinan derivatives as peripheral selective μ opioid receptor agents
Yuan, Yunyun,Elbegdorj, Orgil,Chen, Jianyang,Akubathini, Shashidhar K.,Zhang, Feng,Stevens, David L.,Beletskaya, Irina O.,Scoggins, Krista L.,Zhang, Zhenxian,Gerk, Phillip M.,Selley, Dana E.,Akbarali, Hamid I.,Dewey, William L.,Zhang, Yan
, p. 10118 - 10129 (2013/01/16)
Peripheral selective μ opioid receptor (MOR) antagonists could alleviate the symptoms of opioid-induced constipation (OIC) without compromising the analgesic effect of opioids. However, a variety of adverse effects were associated with them, partially due to their relatively low MOR selectivity. NAP, a 6β-N-4′-pyridyl substituted naltrexamine derivative, was identified previously as a potent and highly selective MOR antagonist mainly acting within the peripheral nervous system. The noticeable diarrhea associated with it prompted the design and synthesis of its analogues in order to study its structure-activity relationship. Among them, compound 8 showed improved pharmacological profiles compared to the original lead, acting mainly at peripheral while increasing the intestinal motility in morphine-pelleted mice (ED50 = 0.03 mg/kg). The slight decrease of the ED50 compared to the original lead was well compensated by the unobserved adverse effect. Hence, this compound seems to be a more promising lead to develop novel therapeutic agents toward OIC.
NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS
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Page/Page column 62, (2010/08/08)
Selective, non-peptide antagonists of the ma opioid receptor { MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.
