Category: 801282-00-8

Application of 801282-00-8, These common heterocyclic compound, 801282-00-8, name is 2-Fluoro-3-methoxyaniline, 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.

[00385] Intermediate 30. l-(3-Chloro-2-fluorophenyl)-5-methoxy-lH-l,2,3-triazole-4- carboxylic acid: To a solution of 2-fluoro-3-methoxyaniline (1 g, 7.09 mmol) in TFA (10 mL) and water (5 mL) at 0 C was added an aq. solution of NaN02 (0.733 g, 10.63 mmol) dropwise. The resulting mixture was stirred at 0 C for 0.5 h and NaN3 (0.921 g, 14.17 mmol) was added portionwise. The reaction mixture was gradually warmed to rt and stirred for 4 h. The reaction was quenched with water (150 mL) and extracted with EtOAc (2×100 mL). The organic layer was washed with sodium phosphate solution (10%) and brine (50 mL), dried, and concentrated. The resulting brown oil was re- dissolved in DMSO (20 mL) and added t-butylpropiolate (1 mL) followed by K2CO3 (1 g), Cu(OAc)2 (0.2 g), and sodium ascorbate (100 mg). The resulting mixture was stirred at rt overnight. The reaction was quenched with water (200 mL) and extracted with EtOAc (2 x 100 mL). The organic layer was dried and concentrated. The residue was purified by silica gel chromatography to yield the desired product as brown oil. 1H NMR (400 MHz, CDCI3) delta 13.19 (br. s., 1H), 7.36 – 7.20 (m, 2H), 7.17 – 6.95 (m, 1H), 6.76 (td, J = 8.1, 1.3 Hz, 1H), 3.91 (s, 3H), 1.74 – 1.49 (m, 10H). MS(ESI) m/z: 238.0 (M+H)+.

The synthetic route of 801282-00-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; PINTO, Donald J.; CORTE, James R.; GILLIGAN, Paul J.; FANG, Tianan; SMITH II, Leon M.; WANG, Yufeng; YANG, Wu; EWING, William R.; WO2013/22818; (2013); A1;,
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Some common heterocyclic compound, 801282-00-8, name is 2-Fluoro-3-methoxyaniline, molecular formula is C7H8FNO, 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. Recommanded Product: 2-Fluoro-3-methoxyaniline

Aniline D3 (1.18 g, 8.36 MMOL) was combined with dimethylacetylene dicarboxylate A3 (1.45 mL, 10.0 MMOL) in methanol (25 mL). The reaction was REFLUXED for 2 hours before being concentrated to dryness. The crude material was purified by flash chromatography eluting with 9/1 (hexane/EtOAc) to give the Michael adduct D4 as a yellow oil, (1. 27 g, 54%)

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 801282-00-8, its application will become more common.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH & CO KG; WO2004/103996; (2004); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Application of 801282-00-8, The chemical industry reduces the impact on the environment during synthesis 801282-00-8, name is 2-Fluoro-3-methoxyaniline, I believe this compound will play a more active role in future production and life.

2,2-dimethyl-l ,3-dioxane-4,6,-dione (4.58 g, 31.78mmol) in trimethyl orthoformate (27.3mL, 245.9 mmol) was refiuxed at 100 C for 1 hr. 2-fluoro-3-methoxyaniline (3.9 g, 27.63 mmol) was then added and refluxing was continued for an additional hour. The reaction was cooled to room temperature and the suspension was filtered. The solid was washed with MeOH (60 mL) and dried under vacuum to yield the title compound. XH NMR H20438-004-04 (400MHz, chloroform-d) delta= 1 1.36 – 1 1.38 (m, 1H), 8.63-8.60 (m, 1H), 7.26- 6.83 (m, 3H), 3.92 (s, 3H), 1.75 (s, 6H).

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, 2-Fluoro-3-methoxyaniline, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; MERCK SHARP & DOHME CORP.; CALDWELL, John, P.; CAPLEN, Mary Ann; CUMMING, Jared, N.; DYKSTRA, Kevin, D.; HRUZA, Alan; LANKIN, Claire; LI, Derun; LIU, Hong; MCCRACKEN, Amy; MCKITTRICK, Brian; RAO, Ashwin; TAGAT, Jayaram, R.; TANG, Haiqun; TAOKA, Brandon, M.; VERRAS, Andreas; WALSH, Shawn, P.; WU, Wen-Lian; ZHANG, Tianyuan; (132 pag.)WO2018/34917; (2018); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Reference of 801282-00-8, These common heterocyclic compound, 801282-00-8, name is 2-Fluoro-3-methoxyaniline, 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.

00157] Preparation of compound 10[00158] To a solution of compound 9 (13 g, 92 mmol) in DMF (100 mL) was added a solution of NBS (16.4 g, 92 mmol, 1.0 eq) in DMF (100 mL) drop-wise. The reaction mixture was stirred at room temperature for 3h, then diluted with ethyl acetate (500 mL) and washed with brine (2xl50mL). The organic phase was dried (Na2S04), filtered and concentrated to give the title compound 10 as brown oil (23 g, 98% yield). ESI-MS (M+H) : 219.9.

Statistics shows that 2-Fluoro-3-methoxyaniline is playing an increasingly important role. we look forward to future research findings about 801282-00-8.

Reference:
Patent; SUZHOU KINTOR PHARMACEUTICALS,INC.; TONG, Youzhi; WO2012/119559; (2012); A1;,
Ether – Wikipedia,
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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. 801282-00-8, name is 2-Fluoro-3-methoxyaniline, A new synthetic method of this compound is introduced below., Safety of 2-Fluoro-3-methoxyaniline

Preparation of compound 10[00177] To a solution of compound 9 (13 g, 92 mmol) in DMF (100 mL) was added a solution of NBS (16.4 g, 92 mmol, 1.0 eq) in DMF (100 mL) drop-wise. The reaction mixture was stirred at room temperature for 3h, then diluted with ethyl acetate (500 mL) and washed with brine (2xl50mL). The organic phase was dried (Na2S04), filtered and concentrated to give the title compound (10) as brown oil (23 g, 98%) yield). ESI-MS (M+H)+: 219.9.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; TONG, Youzhi; WO2011/29392; (2011); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem