How is Risdiplam synthesised?
Synthesis of Risdiplam
The SNAr reaction between amine 194 and bromopyridine 195 furnished 196 in good yield. Nitro reduction via hydrogenation in the presence of a platinum catalyst preceded treatment with di-tert-butyl malonate in anisole at elevated temperatures to give pyridopyrimidone 197 in high overall yield over the two steps. Tosylation formed sulfonate 198, which then participated in a Suzuki coupling with 200 (which originated from aryl chloride 199 via Miyaura coupling) to establish the framework of risdiplam. Risdiplam was formed after N-Boc deprotection of 201 with n-propanolic HCl and was isolated after pH adjustment.
Introduction of Risdiplam
Risdiplam was approved by the USFDA for the treatment of spinal muscular atrophy caused by a mutation leading to a deficiency in the survival motor neuron (SMN) protein. It is an orally administered SMN2-directed RNA splicing modifier that acts by activating an alternative gene SMN2 to produce full-length and functional SMN protein. This medication was developed by Roche, PTC Therapeutics Inc., and the SMA Foundation.
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![1825352-65-5 Risdiplam](/ProductImageEN/2023-10/Small/234866c2-d750-4616-80ff-fffbf1d4f542.jpg)
US $0.00/kg2024-07-18
- CAS:
- 1825352-65-5
- Min. Order:
- 1kg
- Purity:
- 0.99
- Supply Ability:
- 20tons
![1825352-65-5 Risdiplam](/ProductImageEN/2024-06/Small/7f5eb091-33b8-416c-bdfa-09a0bc9f70b1.jpg)
US $0.00-0.00/g2024-06-24
- CAS:
- 1825352-65-5
- Min. Order:
- 1g
- Purity:
- 99.5%min
- Supply Ability:
- 1000g