150085-44-2Relevant articles and documents
Discovery of melanin-concentrating hormone receptor R1 antagonists using high-throughput synthesis
Su, Jing,McKittrick, Brian A.,Tang, Haiqun,Czarniecki, Michael,Greenlee, William J.,Hawes, Brian E.,O'Neill, Kim
, p. 1829 - 1836 (2005)
A structure-activity study on benzylpiperidine 1 was accomplished by utilizing high-throughput synthesis. Three focused libraries were designed and synthesized to quickly develop SAR. Further optimization led to the discovery of compound 2, an MCH receptor R1 antagonist with over 400-fold improvement in biological activity over the original lead.
Tuning the Circular Dichroism and Circular Polarized Luminescence Intensities of Chiral 2D Hybrid Organic–Inorganic Perovskites through Halogenation of the Organic Ions
Chao, Yu-Chiang,Chen, Deng-Gao,Chiu, Ching-Wen,Chou, Pi-Tai,Lin, Jin-Tai,Lin, Tai-Chun,Liu, Yi-Hung,Yang, Lan-Sheng
, p. 21434 - 21440 (2021)
Through the incorporation of various halogen-substituted chiral organic cations, the effects of chiral molecules on the chiroptical properties of hybrid organic–inorganic perovskites (HOIPs) are investigated. Among them, the HOIP having a Cl-substituted chiral cation exhibits the highest circular dichroism (CD) and circular polarized luminescence (CPL) intensities, indicating the existence of the largest rotatory strength, whereas the F-substituted HIOP shows the weakest intensities. The observed modulation can be correlated to the varied magnetic transition dipole of HOIPs, which is sensitive to the d-spacing between inorganic layers and the halogen–halogen interaction between organic cations and the inorganic sheets. These counteracting effects meet the optimal CD and CPL intensity with chlorine substitution, rendering the rotatory strength of HOIPs arranged in the order of (ClMBA)2PbI4>(BrMBA)2PbI4>(IMBA)2PbI4>(MBA)2PbI4>(FMBA)2PbI4.
Monoamine oxidase-ω-transaminase cascade for the deracemisation and dealkylation of amines
O'Reilly, Elaine,Iglesias, Cesar,Turner, Nicholas J.
, p. 992 - 995 (2014/05/06)
Herein we report a one-pot protocol for the deracemisation of chiral benzylic amines employing a novel monoamine oxidase-ω-transaminase cascade, allowing access to enantiopure compounds in >99 % ee. We also demonstrate that the same enzymatic cascade can be employed for the dealkylation of secondary amines with >99 % conversion. Cascade ball: A monoamine oxidase- ω-transaminase cascade has been developed for the deracemisation of chiral benzylic amines, allowing access to the enantiopure compounds in >99 % ee. The same system was also employed for the efficient dealkylation of secondary amines.
RADIOPHARMACEUTICAL PRODUCTS FOR DIAGNOSIS AND THERAPY OF ADRENAL CARCINOMA
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, (2014/04/17)
A radiopharmaceutical composition is disclosed comprising novel iodometomidate derivatives of formula (I) which bind specifically to adrenal enzymes and which exhibit an improved stability. The compounds of formula (I) are suitable for use in a diagnostic
Radiopharmaceutical products for diagnosis and therapy of renal carcinoma
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Paragraph 0061-0062, (2014/05/06)
A radiopharmaceutical composition is disclosed comprising novel iodometomidate derivatives of formula (I) which bind specifically to adrenal enzymes and which exhibit an improved stability. The compounds of formula (I) are suitable for use in a diagnostic
Halogen-bonding interaction stabilizing cluster-type diastereomeric salt crystals
Kobayashi, Yuka,Maeda, Jin,Ando, Tetsuo,Saigo, Kazuhiko
experimental part, p. 685 - 690 (2011/10/09)
O-Ethyl 4-chlorophenylphosphonothioic acid (1) was newly synthesized and applied as a chiral selector for the enantioseparation of racemic l-(4-halophenyl)ethylamines (halo = F, Cl, Br, I; 2a-d) through diastereomeric salt formation. The phosphonothioic acid 1 showed an excellent chirality-recognition ability for the fluorinated and iodinated amines 2a and 2d with the dramatic switch of the absolute configuration of the enantio-enriched isomers in the deposited salts from R for the amine 2a to S for the amine 2d. The X-ray crystallographic analyses of the four pairs of diastereomeric salts revealed that halogen-bonding interaction in the salt crystals plays a very important role for the switch.