Category: 1252934-30-7

Application of 1252934-30-7,Some common heterocyclic compound, 1252934-30-7, name is 3-(Bromomethyl)-1,1-difluorocyclobutane, molecular formula is C5H7BrF2, 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.

3 -(Bromomethyl)- 1,1 -difluoro-cyclobutane (505 mg, 2.73 mmol) was added dropwisc over 15 mm, to a mixture of tert-butyl 4,6-dihydro-2H-pyrrolo[3,4- c]pyrazole-5-carboxylate (560 mg, 2.67 mmol), cesium carbonate (1.39 g, 4.28 mmol) and DMF (5 mL) at 0 C. The reaction mixture was allowed to warm to ambient temperature and stirred for 18 h. The solvent was concentrated and the material was partitioned betweenwater (50 mL) and EtOAc. The aqueous layer was washed with EtOAc (2 x 30 mL). The combined organic layers were washed with brine, dried (MgSO4), and the solvent was concentrated. Purification (FCC, Si02 using ether) provided the title compound (344 mg, 41%). ?H NMR (300 MHz, CDC13) 3 = 7.10 (d, J = 10.0 Hz, 1H), 4.50 -4.37 (m, 4H), 4.18 (d, J = 5.5 Hz, 2H), 2.78-2.56 (m, 3H), 2.47-2.25 (m, 2H), 1.50 (s, 9H); [M+H] = 314.26.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3-(Bromomethyl)-1,1-difluorocyclobutane, its application will become more common.

Reference:
Patent; DART NEUROSCIENCE, LLC; BASINGER, Jillian; BOOKSER, Brett; CHEN, Mi; CHUNG, DeMichael; GUPTA, Varsha; HUDSON, Andrew; KAPLAN, Alan; NA, James; RENICK, Joel; SANTORA, Vincent; WO2015/164520; (2015); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 1252934-30-7, name is 3-(Bromomethyl)-1,1-difluorocyclobutane, A new synthetic method of this compound is introduced below., Recommanded Product: 3-(Bromomethyl)-1,1-difluorocyclobutane

10570] To 2.lh (18 mg, 0.047 mmol) was added DMF (Volume: 0.5 mE) and cesium carbonate (53.8 mg, 0.165 mmol). The reaction was stirred at room temperature for 5 minutes then 3-(bromomethyl)-1 , 1 -difluorocyclobutane (21. 83 mg, 0.118 mmol) was added. The reaction was heated to70 C. and stirred for 3 hours or until done by ECMS. The reaction was cooled, 0.5 ml of DMF was added, then filtered through a 0.45 nM in line filtet The DMF solution with the desired product 2.39a was used as is for the next step, assume quantitative yield. EC-MS (mlz): 486.4 [M+H], 0.92 mm.

The synthetic route of 1252934-30-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Novartis AG; FU, Jiping; HAN, Wooseok; KARUR, Subramanian; LU, Peichao; PFISTER, Keith Bruce; YOUNG, Joseph Michael; (97 pag.)US2018/312507; (2018); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

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;,
Bromide – Wikipedia,
bromide – Wiktionary