13826-35-2Relevant articles and documents
Ullman Ether Synthesis in DMI. Preparation of m-Phenoxybenzyl Alcohol
Oi, Ryu,Shimakawa, Chitoshi,Takenaka, Shinji
, p. 899 - 900 (1988)
The condensation of m-hydroxybenzyl alcohol with chlorobenzene was examined in several different solvents, and an effective route to m-phenoxybenzyl alcohol has been developed by using 1,3-dimethyl-2-imidazolidinone (DMI) as a solvent.
Improving metabolic stability with deuterium: The discovery of HWL-066, a potent and long-acting free fatty acid receptor 1 agonists
Liu, Chunxia,Li, Zheng,Shi, Wei,Li, Huilan,Wang, Nasi,Dai, Yuxuan,Liao, Chen,Huang, Wenlong,Qian, Hai
, p. 1547 - 1554 (2018)
The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancing of glucose-stimulated insulin secretion. The FFA1 agonist GW9508 has great potential for the treatment of type 2 diabetes mellitus, but it has been suffering from high plasma clearance probably because the phenylpropanoic acid is vulnerable to β-oxidation. To identify orally available analog without influence on the unique pharmacological mechanism of GW9508, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the α-position of phenylpropionic acid affording compound 4 (HWL-066). As expected, HWL-066 revealed a lower clearance (CL?=?0.23?L?1?hr?1?kg?1), higher maximum concentration (Cmax?=?5907.47?μg/L), and longer half-life (T1/2?=?3.50?hr), resulting in a 2.8-fold higher exposure than GW9508. Moreover, the glucose-lowering effect of HWL-066 was far better than that of GW9508 and comparable with TAK-875. Different from glibenclamide, no side-effect of hypoglycemia was observed in mice after oral administrating HWL-066 (80?mg/kg).
Phenylpropiolic acid small molecular organic compounds and synthetic method and application thereof
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Paragraph 0070; 0071; 0072, (2019/04/13)
The invention relate to a category of novel phenylpropiolic acid small molecular organic compounds as shown in a structural formula (I) or stereisomers, crystals, hydrates or pharmaceutically acceptable salt and an application of the phenylpropiolic acid small molecular organic compounds or stereisomers, crystals, hydrates or pharmaceutically acceptable salt and pharmaceutical compositions comprising the compounds in preparing a GPR40 agonist and drugs for promoting insulin release, treating and/or preventing diabetes or complications, treating diabetes inducing poor therapeutic effect inducedby acquired drug-resistance and complications and the like. The invention also provides a preparation method of the phenylpropiolic acid small molecular organic compounds as shown in the structural formula (I). The phenylpropiolic acid small molecular organic compounds have good anti-diabetes effect and the risk of inducing hypoglycemia is lower than that of conventional drugs.
Methanol as hydrogen source: Transfer hydrogenation of aromatic aldehydes with a rhodacycle
Aboo, Ahmed H.,Bennett, Elliot L.,Deeprose, Mark,Robertson, Craig M.,Iggo, Jonathan A.,Xiao, Jianliang
supporting information, p. 11805 - 11808 (2018/11/10)
A cyclometalated rhodium complex has been shown to perform highly selective and efficient reduction of aldehydes, deriving the hydrogen from methanol. With methanol as both the solvent and hydrogen donor under mild conditions and an open atmosphere, a wide range of aromatic aldehydes were reduced to the corresponding alcohols, without affecting other functional groups.
