Some common heterocyclic compound, 16034-46-1, name is 1-Methyl-1H-pyrazole-5-carboxylic acid, molecular formula is C5H6N2O2, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Safety of 1-Methyl-1H-pyrazole-5-carboxylic acid
42-1 : 1 -Methyl-N-4-[rel-(4aS,5aS)-5a-methyl-4-oxo-3-(phenylamino)-1 ,4,4a,5,5a,6- hexahydrocyclopropa[f]indol-2-yl]pyridin-2-yl-1 H-pyrazole-5-carboxamide A solution of 1 -methyl-1 H-pyrazole-5-carboxylic acid (1 10 mg, 871 muiotaetaomicronIota) and HATU (331 mg, 871 muiotaetaomicronIota) in DMA (3 mL) was added to a mixture of rel-(4aR,5aR)-2-(2-Aminopyridin- 4-yl)-3-anilino-5a-methyl-4a,5,5a,6-tetrahydrocyclopropa[f]indol-4(1 H)-one (26; 100 mg, 290 muiotaetaomicronIota) and DIPEA (152 muIota_, 871 muiotaetaomicronIota) in DMA (3 mL) and stirred for 16 h at 50. The mixture was concentrated, DCM added and washed with water and dried over sodium sulfate. After filtration and concentration the residue was purified by Biotage (SNAP NH 28 g, EtOH:DCM) to give the title compound (91 mg, 69%).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 16034-46-1, its application will become more common.
Reference:
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; GRAHAM, Keith; KLAR, Ulrich; BRIEM, Hans; SIEMEISTER, Gerhard; MOeNNING, Ursula; (145 pag.)WO2017/21348; (2017); A1;,
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