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. 1252934-30-7, name is 3-(Bromomethyl)-1,1-difluorocyclobutane belongs to bromides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. 1252934-30-7
Ethyl (R)-12-hydroxy-l l-methoxy-3,3-dimethyl-8-oxo-2,3,8,13b-tetrahydro-lH-pyrido[2,l- a]pyrrolo[l,2-c]phthalazine-7-carboxylate (59 mg, 150 muetaiotaomicron) was combined with 3- (bromomethyl)-l,l-difluorocyclobutane (85 mg, 460 mumol) and Potassium Carbonate (85 mg, 0.61 mmol) in DMF (0.4 mL). The mixture was stirred at 70 C for 55 minutes, and then cooled to room temperature. Aqueous 1M lithium hydroxide (334 mu) was added and the mixture was stirred at 35 C for 30 minutes. The mixture was cooled to room temperature, diluted with TFA, and purified by preparative HPLC to provide (R)-12-((3,3-difluorocyclobutyl)methoxy)-l l- methoxy-3,3-dimethyl-8-oxo-2,3,8,13b-tetrahydro-lH-pyrido[2,l-a]pyrrolo[l,2-c]phthalazine-7- carboxylic acid as a TFA salt. l NMR (400 MHz, Acetonitrile-d3) delta 8.45 (s, IH), 7.39 (s, IH), 7.26 (s, IH), 6.95 (d, J = 0.9 Hz, IH), 4.84 (d, J = 6.2 Hz, IH), 4.16 (qt, J = 12.8, 6.5 Hz, 2H), 3.92 (s, 3H), 2.85 – 2.33 (m, 7H), 1.89 (ddd, J = 12.6, 7.8, 2.7 Hz, IH), 1.62 (ddd, J = 12.4, 10.8, 7.8 Hz, IH), 1.36 (s, 3H), 0.66 (s, 3H). 19F NMR (376 MHz, Acetonitrile-d3) delta -77.33 , -84.17 – -85.00 (m), -93.89 – -94.83 (m). MS (m/z) 461.3 [M+H]+.
The synthetic route of 1252934-30-7 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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