《Development and Process Intensification of an Efficient Flow-Cascade Reaction Sequence in the Synthesis of Afizagabar》 was written by Petho, Balint; Szilagyi, Gabor B.; Mengyel, Bela; Nagy, Tamas; Farkas, Ferenc; Katai-Fadgyas, Katalin; Volk, Balazs. Synthetic Route of C10H7FO2S And the article was included in Organic Process Research & Development on April 15 ,2022. The article conveys some information:
The traditional, batchwise pilot plant manufacturing process of a key intermediate drug candidate afizagabar (S44819) involved several kinds of transformations (besides a Dakin-West-type reaction, a ring closure and a keto reduction step). To mitigate some of the hazards associated with this sequence, a flow chem. approach was developed. First, a flow-cascade process was elaborated, which furnished the product with a throughput of 1.52 g/h with a HPLC purity of 95.6%. The bottleneck of the procedure in terms of output was the heterogeneous catalytic hydrogenation, therefore subsequent process intensification efforted primarily concentrated on this step. Finally, application of higher concentrations and an upscaled hydrogenation reactor combined with the corresponding adjustment of parameters of further reaction steps resulted in an efficient process with an effective product yield of 11.95 g/h and an increased HPLC purity (97.1%). The 4-step uninterrupted process described here was based on a newly developed heterogeneous flow reactor system and a custom-made liquid-liquid extractor, providing an instructive case study on handling hazardous processes in a safe and efficient way. After reading the article, we found that the author used Methyl 4-fluorobenzo[b]thiophene-2-carboxylate(cas: 220180-55-2Synthetic Route of C10H7FO2S)
Methyl 4-fluorobenzo[b]thiophene-2-carboxylate(cas: 220180-55-2) belongs to benzothiophene.Benzothiophene is a fused ring compound of thiophene ring and benzene ring, which is an important class of heterocycles with advantageous structures. Synthetic Route of C10H7FO2SIt has been used as a raw material for the synthesis of biologically active structures and is found in pharmaceuticals such as selective estrogen receptor modulators, leukotriene synthesis inhibitors and antifungals, as well as in many natural products.
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem