Category: 261762-59-8

Electric Literature of 261762-59-8 ,Some common heterocyclic compound, 261762-59-8, molecular formula is C7H6ClFO, 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.

To a solution of the compound of Reference Example 1 (100 mg, 0.32 mmol) in 1,4-dioxane (0.64 mL) was added (2-chloro-5-fluorophenyl) methanol (120 mg, 0.74 mmol), sodium hydride , 0.80 mmol) at room temperature, and the mixture was stirred at 100 C. for 48 hours. Water (10 mL) was added to the reaction mixture at room temperature and extracted with ethyl acetate (10 mL × 2). The organic layers were combined, dried over sodium sulfate and concentrated. The resulting concentrate was purified by silica gel column chromatography (eluent: ethyl acetate / n-hexane = 30/70) to give an intermediate as a yellow oil (80 mg).To a solution of the obtained intermediate (80 mg) in 1,4-dioxane (0.32 mL) was added 4 N hydrogen chloride 1,4-dioxane solution (0.8 mL) at room temperature, and the mixture was stirred at room temperature for 1 hour. Acetonitrile (5.0 mL) was added to the reaction mixture at room temperature, diethyl ether (1.5 mL) was added dropwise at room temperature, and the mixture was stirred at room temperature for 1 hour. The solid was collected by filtration and dried under reduced pressure at room temperature to give 1- (6 – ((2-chloro-5-fluorobenzyl) oxy) pyrazin-2-yl) -1, 4- diazepane dihydrochloride Compound of Example 8) as a white solid (40 mg, 31% yield).

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 261762-59-8, 2-Chloro-5-fluorobenzyl alcohol, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; TORAY INDUSTRIES INCORPORATED; KIKUCHI, TSUKASA; OKANO, TSUBASA; (24 pag.)JP2017/14121; (2017); A;,
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Electric Literature of 261762-59-8, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 261762-59-8, name is 2-Chloro-5-fluorobenzyl alcohol. This compound has unique chemical properties. The synthetic route is as follows.

The solution of 2-chloro-5-fluoro-benzoic acid (4.00 g, 23.0 mmol) in THE (200 ml) was added triethylamine (4.14 ml, 29.9 mmol). At -30 C, the mixture was added ethyl chloroformate (2.62 ml, 27.8 mmol) and stirred for 10 min. The solution was added sodium borohydrate (2.60 g, 68.9 mmol) and stirred for 5 min. The mixture was added H2O (10 ml) and stirred for 20 min at room temperature. The solution was concentrated in vacuo and the residue was added CHCl3 and 1 N HClaq. The organic layer was washed with 1 N NaOHaq and dried over Na2SO4. The solution was removed in reduced pressure. The residue was washed with n-hexane to give alcohol as a colorless solid. To the CH2Cl2 suspention of dimethylsulfoxide (2.43 ml, 34.2 mmol) was added a solution of oxalyl chloride (1.47 ml, 17.1 mmol) in 50 ml of dry CH2Cl2 at -78 C, and the resulting mixture was stirred for 20 min. CH2Cl2 (15 ml) solution of the alcohol was added at -78 C. The mixture was allowed to warm to -40 C for 1 h. The mixture was added triethylamine (7.89 ml, 57.0 mmol), allowed to warm to room temperature, and was treated with 0.1 N HClaq. The organic layer was washed with saturated Na2CO3aq, dried over Na2SO4, and concentrated in vacuo to give the title compound (1.33 g, 37%) as a colorless solid after trituration with n-hexane. 1H NMR (400 MHz, CDCl3) delta 7.22-7.28 (1H, m), 7.41-7.47 (1H, m), 7.58-7.64 (1H, m), 10.42 (1H, d, J = 3.2 Hz). MS (EI) m/z 158 M+.

According to the analysis of related databases, 261762-59-8, the application of this compound in the production field has become more and more popular.

Reference:
Article; Ichikawa, Masanori; Yokomizo, Aki; Itoh, Masao; Sugita, Kazuyuki; Usui, Hiroyuki; Shimizu, Hironari; Suzuki, Makoto; Terayama, Koji; Kanda, Akira; Bioorganic and Medicinal Chemistry; vol. 19; 6; (2011); p. 1930 – 1949;,
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Synthetic Route of 261762-59-8 , The common heterocyclic compound, 261762-59-8, name is 2-Chloro-5-fluorobenzyl alcohol, molecular formula is C7H6ClFO, 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.

Conversion 4, step 4C; Preparation of 5-(2-chloro-5-fluoro-benzyloxy)-3-{4-(4-methyl-piperazin-1-yl)-2-[(tetrahydro-pyran-4-yl)-(2,2,2- trifluoro-acetylj-aminol-benzoylaminoj-indazole-i-carboxylic acid tert-butyl ester; Triphenylphosphine (146 mg, 0.557 mmol) in DCM (2 mL), cooled at 4C, in a nitrogen atmosphere was treated with neat diisopropyl azodicarboxylate (0.106 mL, 0.5208 mmol) while stirring. After 20 minutes the colourless solution was treated with 5-hydroxy-3-{4-(4-methyl-piperazin-1-yl)-2-[(tetrahydro-pyran-4-yl)-(2,2,2-trifluoro-acetyl)-amino]- benzoylamino}-indazole-1-carboxylic acid tert-butyl ester (82 mg, 0.5108 mmol) in DCM (2 mL). After 2 hours the crude was purified by flash chromatography over silica gel (DCM:EtOH:35% NH4OH 95:5:0.5) and 108 mg of title compound were obtained as a white solid in 59 % yield. ESI(+) MS: m/z 790 (MH+).

The synthetic route of 261762-59-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NERVIANO MEDICAL SCIENCES S.r.l.; MENICHINCHERI, Maria; BERTRAND, Jay, Aaron; MARCHIONNI, Chiara; NESI, Marcella; ORSINI, Paolo; PANZERI, Achille; WO2010/69966; (2010); A1;,
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