Category: 166599-84-4

166599-84-4, Benzofuran-4-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(RS)-2-Cyclopropyl-2-[methyl-(2-methyl-5-phenyl-thiazole-4-carbonyl)-amino]-ethyl- ammonium chloride (0.17 mmol, 1.0 eq.) was suspended in DMF (0.2 ml) and a solution of benzofuran-4-carboxylic acid (0.135 mmol, 0.79 eq.) and DIPEA (0.57 mmol, 3.4 eq.) in DMF (0.54 ml) was added. Finally a solution of HATU (0.135 ml, 0.79 eq.) was added and the mixture was shaken overnight. The solvent was stripped off and the residue was purified by preparative HPLC yielding the desired product (0.0134 g, 22%)LC-MS: tR = 0.99; [M+H]+ = 460.18, 166599-84-4

166599-84-4 Benzofuran-4-carboxylic acid 22324117, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; WO2009/22311; (2009); A2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

166599-84-4, Benzofuran-4-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of benzofuran-4-carboxylic acid (Eissenstat M. A. et al, J. Med. Chem. 1995, 38, 16, 3094-3105 (61 mg), PyBOP (196 mg), DIEA (0.15 mL) in dry DMF (0.5 mL), was added a solution of (2RS)-(2-aminomethyl-azetidin-1-yl)-biphenyl-2-yl-methanone (100 mg) in dry DMF (0.5 mL). The resulting reaction mixture was stirred at RT for 20 h. The reaction mixture was diluted with EA, washed with water. The aqueous phase was extracted once again with EA, the combined organic extracts were dried (MgSO4), filtered and concentrated to yield the crude product as light brown oil.FC (EA) gave 140 mg (71%) of the title compound as a light yellow oilLC-MS: rt=0.99 min, 411 [M+H]+., 166599-84-4

As the paragraph descriping shows that 166599-84-4 is playing an increasingly important role.

Reference£º
Patent; Actelion Pharmaceuticals Ltd.; US2010/222600; (2010); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

166599-84-4, Benzofuran-4-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

TBTU (1.24 mmol, 1.05eq) is added to a solution of the respective carboxylic acid (1.18 mmol, l.Oeq), (lS,3S,5S)-3-aminomethyl-2-aza-bicyclo[3.1.0]hexane-2-carboxylic acid tert-butyl ester (1.18 mmol, l.Oeq) and DIPEA (1.77 mmol, 1.5eq) in DCM, DMF or acetonitrile (10 mL). After 2h the mixture is washed with water, hydrochloric acid (0.5 M) and water. The organic layer is dried over Na2SO4, the solvents are removed in vacuo and the residue is purified by prep. HPLC or by flash chromatography (EtO Ac/heptane).(lS,3S,5S)-3-{[(benzofuran-4-carbonyl)-amino]-methyl}-2-aza-bicyclo[3.1.0]hexane-2- carboxylic acid tert-butyl ester prepared by reaction of (lS,3S,5S)-3-aminomethyl-2-aza-bicyclo[3.1.0]hexane-2- carboxylic acid tert-butyl ester with benzofuran-4-carboxylic acid (M.A. Eissenstat et al. J. Med. Chem. 1995, 38, 3094-3105). LC-MS (acidic): tR = 1.00 min; [M+H]+ = 357.1. 1H- NMR (CDCl3): delta = 0.58 (bs, IH); 0.80-0.86 (m, IH); 1.52 (s, 9H); 1.52-1.59 (m, IH); 1.79 (bd, J = 13.3 Hz, IH); 2.51-2.60 (m, IH); 3.24-3.30 (m, IH); 3.60-3.64 (m, 2H); 4.45-4.52 (m, IH); 7.32 (t, J = 7.9 Hz, IH); 7.47 (bs, IH); 7.61 (d, J = 8.2 Hz, IH); 7.65 (d, J = 7.5 Hz, IH); 7.70 (bs, IH); 8.43 (bs, IH).

166599-84-4, As the paragraph descriping shows that 166599-84-4 is playing an increasingly important role.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; WO2008/81399; (2008); A2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.166599-84-4,Benzofuran-4-carboxylic acid,as a common compound, the synthetic route is as follows.

To a mixture of benzofuran-4-carboxylic acid (11 mg), PyBOP (35 mg), DIEA (0.030 mL) in dry DMF (0.15 mL), was added a solution of (2RS)-(2-aminomethyl-azetidin-1-yl)45-(4-fluoro-phenyl)-2-methyl-thiazol-4-A-methanone (20 mg) in dry DMF (0.1 mL). The resulting reaction mixture was stirred at RT for 20 h. The reaction mixture was diluted with EA, washed with water. The aqueous phase was extracted once again with EA, the combined organic extracts were dried (MgSO4), filtered and concentrated to yield a crude light brown oil.FC (EA to DCM/MeOH: 98/2) gave 23 mg (78%) of the title compound as a white solid.LC-MS: rt=0.94 min, 450 [M+H]+.

166599-84-4, The synthetic route of 166599-84-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Actelion Pharmaceuticals Ltd.; US2010/222600; (2010); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem