Reference of 1029413-51-1,Some common heterocyclic compound, 1029413-51-1, name is 4-Amino-1-(1-boc-azetidin-3-yl)-1H-pyrazole, molecular formula is C11H18N4O2, 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.
Example 14: Synthesis of I -(2-(2-(2-((I -(azetidin-3-yl)-I H-pyrazol-4-yl)amino)-5- chloropyrimidin-4-yl)ethyl)phenyl)cyclopropanecarboxamide (14)H2N.O H2NO_ H1BoC_NN/j NH2 + CI N1>A14 A18HNNNY(a) tert-Butyl 3-(4-((4-(2-(1-carbamoylcyclopropyl)phenethyl) -5-chloropyrimidin-2-yI)amino)- 1H-pyrazol- 1-yI)azetidine- 1-carboxylate (A 18) A suspension of 1-(2-(2-(2,5-dichloropyrimidin-4-yl)ethyl)phenyl)cyclopropanecarboxamide A14 (0.100 g, 0.297 mmol), 052003 (0.291 g, 0.892 mmol) and tert-butyl 3-(4-amino-1H-pyrazol-1-yl)azetidine-1-carboxylate (0.142 g, 0.595 mmol) in dioxane (3 mL) was sonicated for 10 minutes. Xantphos(6.9 mg, 12 pmol) and Pd(ll) acetate (1.3 mg, 5.9 pmol) were added to thesuspension and the mixture was irradiated in the microwave for 20 minutes at 120 00 The resulting mixture was adsorbed onto silica gel and purified by columnchromatography (Biotage Isolera, 24 g Si02 cartridge, 0-100% EtOAc in petroleum benzine 40-60 00 then 0-40% MeOH in EtOAc) to give the title compound A18 as ayellow oil (110 mg, 69%). LCMS-A: rt 6.349 mm; m/z 538.3 [M+H].
The synthetic route of 1029413-51-1 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; CANCER THERAPEUTICS CRC PTY LIMITED; FOITZIK, Richard Charles; MORROW, Benjamin Joseph; HEMLEY, Catherine Fae; LUNNISS, Gillian Elizabeth; CAMERINO, Michelle Ang; GANAME, Danny; STUPPLE, Paul Anthony; LESSENE, Romina; KERSTEN, Wilhelmus Johannes Antonius; HARVEY, Andrew John; HOLMES, Ian Peter; WO2014/26243; (2014); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics