On November 29, 2001, Astles, Peter C.; Eastwood, Paul R.; Houille, Olivier; Levell, Julian; Pauls, Heinz; Czekaj, Mark; Liang, Guyan; Gong, Yong; Pribish, James; Neuenschwander, Kent published a patent.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene The title of the patent was Preparation of (hetero)arylacyl-piperidinyl-benzylamines for use as tryptase inhibitors. And the patent contained the following:
Title compounds I [Ar = (hetero)aryl, where the two groups on the Ar ring are β to each other; R1-2 = H, alkyl; R3 = (un)substituted(hetero)aryl, arylalkenyl, cycloalkenyl, cycloalkyl, etc.; R4 = H, acyl, alkoxy, alkyloxycarbonyl, carboxy, CN, halo, etc.; n = 0 – 4] were prepared Over 300 synthetic examples were disclosed. For instance, 3-bromobenzylbromide was converted in two steps to boronate II. II was coupled to the triflate ester derivative of the enol of 4-oxo-N-benzyloxycarbonylpiperidine (DMF, K2CO3, PdCl2(dppf)•CH2Cl2, 80°C, 18 h) to give the corresponding bicyclic intermediate. This intermediate was deprotected and reduced to the piperidine (EtOH, 10% Pd-C/H2, room temperature, 5 h) and coupled to 5-phenethylthiophene-2-carboxylic acid (DMF, HAPyU, iPr2NEt, room temperature, 18 h) to give III. III had Ki = 50 nM for tryptase. I are useful in the treatment of e.g., asthma and inflammatory diseases. The experimental process involved the reaction of 2-Bromo-4-(bromomethyl)-1-methylbenzene(cas: 259231-26-0).Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene
The Article related to piperidinylbenzylamine tryptase inhibitor preparation, pyridine quinoline thiophene furan indole piperidine tryptase inhibitor preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 2-Bromo-4-(bromomethyl)-1-methylbenzene
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary