{"id":6139,"date":"2021-09-02T03:42:17","date_gmt":"2021-09-01T19:42:17","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=6139"},"modified":"2021-09-02T03:42:17","modified_gmt":"2021-09-01T19:42:17","slug":"2-sep-21-news-introduction-of-a-new-synthetic-route-about-27258-33-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=6139","title":{"rendered":"2-Sep-21 News Introduction of a new synthetic route about 27258-33-9"},"content":{"rendered":"<p><a href=\"https:\/\/www.ambeed.com\/products\/27258-33-9.html\">Application of 27258-33-9<\/a>, These common heterocyclic compound, 27258-33-9, name is 1-Methyl-1H-pyrazole-5-carbaldehyde, its 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.<\/p>\n<p>(l-{4-[5-Amino-2-(3-trifluoromethoxy-phenyl)-pyrimidin-4-yl-amino]- phenyl}-cyclobutyl)-carbamic acid tert-butyl ester (200 mg 0.77 mmol) was dissolved in acetic acid (30 mL), then 2-Methyl-2H-pyrazole-3-carbaldehyde (93.5 mg, 0.85 mmol) and Cu(OAc)2 (140 mg, 0.77 mmol) were added separately. The reaction mixture was stirred at 100 C for 2 h. LC\/MS showed there was about 40% desired product (l-{4-[8-(2-Methyl-2H-pyrazol-3-yl)-2-(3- trifluoromethoxy-phenyl)-purin-9-yl]-phenyl}-cyclobutyl)-carbamic acid tert-butyl ester in the reaction mixture. Then the solvent was removed by concentration, and the residue was dissolved in ethyl acetate (150 mL). The organic layer was washed with sat. NaHC03 aqueous solution, followed by brine, dried over sodium sulfate, filtered and concentrated to give 150 mg of crude desired product with 80% purity, which was used directly without further purification. LC\/MS (ESI+): e\/z: 606.2 [M+l]+.<\/p>\n<p>The synthetic route of 27258-33-9 has been constantly updated, and we look forward to future research findings.<\/p>\n<p>Reference:<br \/><a href=\"http:\/\/v3.espacenet.com\/textdoc?DB=EPODOC&#038;IDX=WO2013078254&#038;F=0\">Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; SKELTON, Nicholas; GRADL, Stefan; BLAKE, James F.; GRAHAM, James M.; GUNAWARDANA, Indrani W.; HENTEMANN, Martin; MARLOW, Allison L.; TANG, Tony P.; WO2013\/78254; (2013); A1;<\/a>,<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/p>\n","protected":false},"excerpt":{"rendered":"<p>The synthetic route of 27258-33-9 has been constantly updated, and we look forward to future research findings.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[160,131],"tags":[126],"class_list":["post-6139","post","type-post","status-publish","format-standard","hentry","category-27258-33-9","category-pyrazoles-derivatives","tag-m-w100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - 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