Lim, Chae Jo published the artcile4-Heteroaryl phthalazin-1(2H)-one derivatives as potent melanin concentrating hormone receptor 1 (MCH-R1) antagonists, Related Products of chlorides-buliding-blocks, the publication is Bulletin of the Korean Chemical Society (2012), 33(7), 2389-2392, database is CAplus.
The target compounds, 4-heteroaryl-2-{3-[4-(3-acetamidophenyl)piperidin-1-yl]propyl}phthalazin-1(2H)-ones, were prepared starting from 2-BrC6H4CO2H in 4 steps starting via Li-halo exchange using excess BuLi, followed by acylation with appropriate heteroaroyl esters to give the corresponding 2-heteroaroylbenzoates. The key 4-heteroarylphthalazin-1(2H)-one intermediates were then generated by condensation with N2H4. Subsequent N-alkylation with Cl(CH2)3I using NaH base afforded 2-(3-chloropropyl)4-heteroarylphthalazin-1 (2H)-ones, which were transformed to the target compounds through coupling with N-[3-(4-piperidinyl)phenyl]acetamide in the presence of Na2CO3. The title compounds proved to be potent MCH-R1 antagonists. An extensive SAR study carried out with substances in this family containing C(4) pyridyl and 5-membered heteroaryl groups led to the identification of a 5-chlorothien-2-yl derivative as a highly potent MCH-R1 antagonist. This substance displayed good metabolic stability, no inhibition of CYP450 enzymes, and low hERG binding activity.
Bulletin of the Korean Chemical Society published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Related Products of chlorides-buliding-blocks.
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https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics