Continuously updated synthesis method about 4152-90-3

The synthetic route of 4152-90-3 has been constantly updated, and we look forward to future research findings.

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. 4152-90-3, name is (3-Chlorophenyl)methanamine, A new synthetic method of this compound is introduced below., name: (3-Chlorophenyl)methanamine

5-[3-(3-Chloro-benzylamino)-phenyl]-5-methyl-5,6-dihydro-2H-[l,4]oxazin-3-ylamine a) (RS)- (3-Chloro-benzyl)-[3-(5-methoxy-3-methyl-3,6-dihydro-2H-[l,4]oxazin-3-yl)- phenyl] -amineA dried pressure tube was charged consecutively under a nitrogen atmosphere with a solution of (RS)-3-(3-bromo-phenyl)-5-methoxy-3-methyl-3,6-dihydro-2H [l,4]oxazine (150 mg, 0.5 mmol) in toluene (5 ml), sodium tert-butylate (157 mg, 1.6 mmol), 2-di-tert-butylphosphino-2′,4′,6′- triisopropylbiphenyl (ie/t-butyl-x-phos) (23 mg, 0.1 mmol), tris(dibenzylideneacetone)- dipalladium chloroform complex (17 mg), and 3-chlorobenzylamine (154 mg, 1.1 mmol). The sealed pressure tube was heated at 100 C for 15 hours. After cooling, the reaction mixture was evaporated to dryness and directly purified by chromatography on an Isolute flash NH2 column using a gradient of heptane/ethyl acetate = 100/0 to 50/50 as the eluent. 85 mg (47%) of (RS)- (3-chloro-benzyl)-[3-(5-methoxy-3-methyl-3,6-dihydro-2H-[l,4]oxazin-3-yl)-phenyl]-amine were obtained as a yellow oil. Mass (calculated) C19H21CIN2O2 [344.844]; (found) [M+H]+ = 345.

The synthetic route of 4152-90-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; SIENA BIOTECH S.P.A; ANDREINI, Matteo; GABELLIERI, Emanuele; GUBA, Wolfgang; HILPERT, Hans; MAUSER, Harald; MAYWEG, Alexander V.; NARQUIZIAN, Robert; POWER, Eoin; TRAVAGLI, Massimiliano; WOLTERING, Thomas; WOSTL, Wolfgang; WO2012/98064; (2012); A1;,
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