On June 30, 2014, Kawamura, Madoka; Shiozawa, Fumiyasu; Kakinuma, Hiroyuki; Otake, Kenichi; Matsuda, Daisuke; Kobashi, Yohei; Suga, Yoichiro; Fusegi, Keiko published a patent.Quality Control of 2-Chloro-5-isopropylpyrimidine The title of the patent was Preparation of azaspiroalkane compounds as GPR119 agonists. And the patent contained the following:
The title compounds [I; p = 0-2; q = 1 or 2; ring A = benzene ring or 6-membered heteroaryl; R11-R13 = independently H, halo, carbamoyl, etc.; X = -O- or -NR3-; R3 = H or alkyl; Y = alkanediyl; R2 = alkyl (optionally substituted with cycloalkyl or aryl), alkylsulfonyl, alkylcarbonyl, etc.; or pharmaceutically acceptable salts thereof], useful for the treatment of diabetes, were prepared For example, treatment of tert-Bu 2-(methoxymethylidene)-7-azaspiro[3.5]nonane-7-carboxylate (preparation given) with CF3CO2H/water, reaction with NaH/triethyl phosphonoacetate, hydrogenation, reduction using LiAlH4, reaction with 4-cyano-3-fluorophenol in the presence of N,N,N’,N’-tetramethylazodicarbamide, hydrolysis, and EDCI-mediated amidation with 2-aminoethanol afforded compound (II). In GPR119 agonist activity test, EC50 of II was 9 nM. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Quality Control of 2-Chloro-5-isopropylpyrimidine
The Article related to azaspiroalkane preparation gpr119 agonist, diabetes treatment azaspiroalkane gpr119 agonist, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Quality Control of 2-Chloro-5-isopropylpyrimidine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia