108468-00-4, 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. 108468-00-4, name is 1-(N-Boc-aminomethyl)-4-(aminomethyl)benzene belongs to amides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.
General procedure: A mixture of carboxylic acid (1.0 eq), amine (1.0-1.5 eq), N,N-diisopropylethylamine or triethylamine (1.5-3.0 eq) and a coupling agentsuch as HBTU (2-(1H-benzotriazol-i-yl)-i,i,3,3- tetramethyluronium hexafluorophosphate), HATU (1 -[Bis(dimethylamino)methylene]-i H-i 2,3-triazolo[4,5-b]pyridinium 3-oxidhexafluorophosphate) or HCTU (O-(i H-6-Chlorobenzotriazole-i -yl)1,1 ,3,3-tetramethyluronium hexafluorophosphate (1.0-1.5 eq) in anhydrous solvents such as DMF or DCM was stirred at room temperature for 1-72 h. The product was isolated and purified using one of the following methods: Step 4: Amide coupling of (S)-1 -[(R)-2-(tert-Butoxycarbonyl-methyl-amino)-4-phenyl- butyryl]-pyrrolidine-2-carboxylic acid (280 mg, 0.72 mmol) with 1-(N-boc-aminomethyl)-4-(aminomethyl)benzene (170 mg, 0.72 mmol) was carried out following General Method I using HATU (330 mg, 0.86 mmol) and DIPEA (0.30 mL, 1 .7 mmol) in DCM (50 mL). Purification by column chromatography (biotage, 0-80% EtOAc/petrol) gave ((R)-1-{(S)-2-[4-(tert- butoxycarbonylamino-methyl)-benzylcarbamoyl]-pyrrolidine-1 -carbonyl}-3-phenyl-propyl)-methyl-carbamic acid tert-butyl ester (230 mg, 51%) as a colourless oil.AnalpH2_MeOH_4MIN: Rt: 3.51 mi mlz 609 [M+H]
The synthetic route of 108468-00-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; UNIVERSITY OF LEEDS; PHILIPPOU, Helen; FOSTER, Richard; FISHWICK, Colin; REVILL, Charlotte; YULE, Ian; TAYLOR, Roger; NAYLOR, Alan; FALLON, Philip, Spencer; CROSBY, Stuart; HOPKINS, Anna; GUETZOYAN, Lucie, Juliette; MACNAIR, Alistair, James; STEWART, Mark, Richard; WINFIELD, Natalie, Louise; (273 pag.)WO2019/186164; (2019); A1;,
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