Reference of 910251-11-5, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 910251-11-5, name is Potassium trifluoro(methoxymethyl)borate belongs to ethers-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
Ethyl (R)-l l-chloro-12-(3-hydroxy-3-methylbut-l-yn-l-yl)-3,3- dimethyl-8-oxo-2,3,8,13b-tetrahydro-lH-pyrido[2,l-a]pyrrolo[l,2-c]phthalazine-7-carboxylate (53 mg, 0.093 mmol) was combined with trifluoro(methoxymethyl)-borane, potassium salt (40 mg, 0.26 mmol), Ruphos Pd G2 (5.1 mg, 0.007 mmol), and potassium carbonate (52 mg, 0.37 mmol) in dioxane:water (5: 1, ImL) under argon in a sealed vial. The mixture was stirred at 110 C for 2.5 hours, after which time it was cooled to 50 C and 1M lithium hydroxide (0.19 ml) was added. The mixture was stirred for 90 minutes, then cooled to room temperature, diluted with TFA and acetonitrile, and purified by preparative HPLC to provide (R)-12-(3-hydroxy-3- methylbut- 1 -yn-1 -yl)- 11 -(methoxymethyl)-3,3-dimethyl-8-oxo-2,3,8, 13b-tetrahydro- 1H- pyrido[2,l-a]pyrrolo[l,2-c]phthalazine-7-carboxylic acid as a TFA salt. XH NMR (400 MHz, Acetonitrile-d3) delta 8.47 (s, 1H), 8.01 (s, 1H), 7.50 (d, J = 1.1 Hz, 1H), 7.29 (s, 1H), 4.88 (d, J = 5.9 Hz, 1H), 4.62 (t, J = 0.8 Hz, 2H), 3.47 (s, 3H), 2.60 – 2.43 (m, 2H), 1.94 – 1.86 (m, 1H), 1.67 – 1.60 (m, 1H), 1.58 (s, 6H), 1.37 (s, 3H), 0.63 (s, 3H). iyF NMR (376 MHz, Acetonitrile- d3) delta -77.28 . MS (m/z) 437.2 [M+H]+.
The synthetic route of Potassium trifluoro(methoxymethyl)borate has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GILEAD SCIENCES, INC.; AKTOUDIANAKIS, Evangelos; CANALES, Eda; CURRIE, Kevin S.; KATO, Darryl; LI, Jiayao; LINK, John O.; METOBO, Samuel E.; SAITO, Roland D.; SCHROEDER, Scott D.; SHAPIRO, Nathan; TSE, Winston C.; WU, Qiaoyin; (262 pag.)WO2018/144605; (2018); A1;,
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