35510-00-0Relevant articles and documents
Preparation method of eluxadoline intermediate
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Paragraph 0051-0055; 0067-0071; 0089-0093, (2018/04/01)
The invention discloses a preparation method of an eluxadoline intermediate. The structure of the intermediate corresponds to a formula IV as shown in the specification. According to the method, 2-halogenated-mesitylene in a formula I serves as a raw material, bromination and cyanation reaction is performed, and finally, the intermediate in the formula IV is obtained. According to the synthesis method, raw materials are inexpensive, easy to obtain and low in cost, scale-up production is facilitated, reaction conditions are mild, and safety coefficient and yield are high.
(S) - 2 - (2,3-dihydrobenzo-furan-3-yl) acetic acid derivatives, its preparation process and its use in medicine
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Paragraph 0128-0130, (2016/10/08)
The invention relates to an (S)-2-(2,3-dihydrobenzofuran-3-radical) acetic acid derivative, a preparation method of the derivative, a medicine composition containing the derivative and the application of the derivative serving as a therapeutic agent, particularly GPR40/FFA1, and particularly provides the (S)-2-(2,3-dihydrobenzofuran-3-radical) acetic acid derivative shown in a general formula (I), and pharmaceutically acceptable salts of the derivative or a prodrug of the derivative. The compound is an agonist of a GPR40/FFA1 receptor and has a good preventive and therapeutic effect on lots of GPR40-mediated diseases, especially diabetes mellitus. The invention also provides a preparation method of the compound.
ANTIDIABETIC TRICYCLIC COMPOUNDS
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Page/Page column 97, (2015/04/28)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
Abundant lattice inclusion phenomenon with sterically hindered and inherently shape-selective tetraarylpyrenes
Moorthy, Jarugu Narasimha,Natarajan, Palani,Venugopalan, Paloth
supporting information; experimental part, p. 8566 - 8577 (2010/03/01)
(Figure Presented) Tetraarylpyrenes H1-H4 that typify molecular systems with orthogonal planes and lack hydrogen bonding functional groups were designed as new host systems with three distinct domains for guest inclusion. In particular, H2 and H4 hosts are found to include a variety of guest molecules. We have determined 42 crystal structures overall (i) to establish the importance of skeletal features of the hosts, (ii) to determine their adaptability in binding diverse guest molecules, and (iii) to delineate favored domains for location of guest molecules and preferred modes of association of the host systems. The unique features of H1-H4 are found to permit binding of aliphatic and aromatic guest species differently: the small-sized guest molecules such as CHCl3, (CH3)2S, etc. are found to be bound in the basin domain, whereas aliphatic and aromatic guests are found to be included in the channel/concave and trough regions, respectively. The crystal structure analyses reveal that as many as 20 out of 28 inclusion compounds of H2 are isostructural with one or more; we have identified 8 different crystal packing types with which each inclusion compound may be associated. The guest-binding potential of host H2 has been exploited to demonstrate the utility of these host systems in (i) the separation of regioisomeric methyl-substituted benzenes and mixtures of cis-trans isomers of decalin, perhydroisoquinoline, and cinnamonitrile, (ii) the stabilization of the keto-enol form of 1,3-diketones, and (iii) the conformational locking of flexible cycloalkanes.
Synthesis of a Novel Series of Arylmethylisothiouronium Derivatives
Tal, Daniel M.,Karlish, Steven J. D.
, p. 3823 - 3830 (2007/10/02)
The bromination by N-bromosucciniminde of various mesitylene derivatives, to produce arylmethyl bromides was compared in different reaction conditions.These compounds are intermediates in the synthesis of arylmethylisothiouronium bromide salts, achieved b
