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◆We speculated that not only B(OMe)3 wasdistilling off, but also H2B(OMe) and HB(OMe)2 whichcould still release hydrogen gas.◆There was a concern that the fluorine onthe piperidine side chain might be cleaved during the DEANB reduction step formingimpurity 42. However, stress tests of the DEANB reduction showed that... 阅9 转0 评0 公众公开 24-08-01 09:07 |
Scalable Synthesis of C5aR1 Antagonist ACT-1014-6470 (2)◆Our first approach for the final steps to ACT-1014-6470(1) relied on the formation of the advanced urea-intermediate 28 from which thecrucial ring closure could be achieved by intramolecular alkylation with theprimary alcohol in an activated form. 阅5 转0 评0 公众公开 24-07-31 10:34 |
Commercial Manufacturing Process for Ipatasertib (2)Chimia, 2021, 75, 605–613. DOI: 10.2533/chimia.2021.605.◆Both key building blocks 2 and 4 are thencoupled in the next step to yield Boc-protected API 11.◆The process performance and robustness hasbeen successfully proven at commercial scale over all ten chemical s... 阅6 转0 评0 公众公开 24-06-30 09:20 |
Protecting-Group-Free Synthesis of MMV693183.◆To complete the synthesis of MMV693183,L-(+)-tartrate salt 18 was reacted with 2,4,5-trifluorobenzoyl chloride (19) inthe presence of 1.5 equiv of Na2CO3, providing the final API in 72% yield in>99 area % (210 nm) purity as determined by HPLC. 阅9 转0 评0 公众公开 24-05-24 18:09 |
Continuous Flow-Facilitated CB2 Agonist Synthesis (1)◆A cannabinoid receptor type 2 (CB2) agonist,RG7774 (5), is currently in a phase II trial for the treatment of diabeticretinopathy. The original route furnished the desired regioisomer of the API 5with poor selectivity (1:1 for the desired isomer). 阅11 转0 评0 公众公开 23-10-16 11:53 |
Highly Diastereoselective Esterification of Ketene...◆Rac-2 was effectively converted into (R)-2 via diastereoselective esterification of ketene in situ generated from the corresponding acyl chloride Rac-17 with (R)-pantolactone followed by hydrolysis of the ester.◆The diastereomeric ratio (dr) of the resulting este... 阅7 转0 评0 公众公开 22-01-10 12:01 |
Highly Diastereoselective Esterification of Ketene...◆Rac-2 was effectively converted into (R)-2 via diastereoselective esterification of ketene in situ generated from the corresponding acyl chloride Rac-17 with (R)-pantolactone followed by hydrolysis of the ester.◆The diastereomeric ratio (dr) of the resulting este... 阅8 转0 评0 公众公开 22-01-10 12:01 |
◆Based on the hypothesis, a catalytic amount of acid was used for this alkylation reactions shown entries 3?5. As expected, the desired reaction was accelerated; in contrast, an unacceptable level of enantiomer (S)-8 was observed. From these results, we could understand that the balance between amount of acid and rea... 阅21 转0 评0 公众公开 21-05-24 14:46 |
