Reference of 25016-20-0, The chemical industry reduces the impact on the environment during synthesis 25016-20-0, name is 1-Methyl-1H-pyrazole-3-carboxylic acid, I believe this compound will play a more active role in future production and life.
Acid R2a (9.3 mg, 0.074 mmol) is dissolved in DCM (2 mL), then TEA (41 mu, 0.295 mmol) is added followed by TBTU (21.7 mg, 0.068 mmol). This solution is stirred for 15 mins, after which the amine hydrochloride Ce (50 mg, 0.059 mmol) is added. The resulting solution is stirred at RT for 16 h and then concentrated. The residual is dissolved in DMSO. The resulting solution is filtered through a Millex filter and purified by prep HPLC (Ammonium formate/MeOH). The pure fractions are combined, concentrated redissolved in MeCN and water, frozen and lyophilized to provide compound 1015.FIA M.S.(electrospray) : 804.5 (M-H)” Retention time (min): 5.2 min1H NMR (400 MHz,DMSO-d6): delta 9.57 (s, 1 H) , 7.76 (d, 1 H, J = 2.4 Hz), 7.67 (bs, 1 H). 7.64 (d, 1 H, J = 9 Hz), 6.88 (d, 1 H, J = 9 Hz), 6.59 (d, 1 H, J = 2.1 Hz), 6.24 (s, 1 H), 5.47 (S, 1 H, J = 6.1 Hz), 5.41-5.31 (m, 3H) 4.81-4.73 (m, 1 H), 4.46 (dd, 1 H, J = 7.8, 7.6 Hz), 4.30-4.13 (m, 2H) 3.90 (s, 3H), 2.46-2.41 (m, 2H), 2.38 (s, 3H), 2.01- 1.69 (m, 4H), 1.59-1.53 (m, 3H), 1.48-1.33 (m, 15H), 1.24-1.12 (m, 4H), 0.64- 0.60(m, 2H)
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, 1-Methyl-1H-pyrazole-3-carboxylic acid, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; LLINAS-BRUNET, Montse; BORDELEAU , Josee; GODBOUT, Cedrickx; LEBLANC, Melissa; MOREAU, Benoit; O’MEARA, Jeffrey; WO2011/63501; (2011); A1;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics