35150-07-3Relevant articles and documents
Synthetic Studies on Alotamide A: Construction of N-Demethylalotamide A
Domínguez, Marta,Román, David,Souto, José A.,de Lera, ángel R.
supporting information, p. 6057 - 6070 (2021/12/10)
Several approaches to the synthesis of cyclodepsipeptide natural product alotamide A are described, eventually affording a very advanced N-demethylated analogue of the targeted natural product. The difficulties found in our endeavors on the synthesis of alotamide A have allowed us to gather some valuable information regarding the most convenient synthetic step for each key transformation. The intramolecular Csp2?Csp2 Stille cross-coupling and the macrolactam formation were found to be reliable protocols for the final construction of the alotamide A skeleton.
Process Development of a Copper(II)-Catalyzed Dehydration of an N -Acyl Prolinal Oxime: Cascade Process and Application at an Elevated Lab Scale
Nonnhoff, Jannis,Gr?ger, Harald
supporting information, p. 4672 - 4677 (2021/10/07)
Chiral N-acyl amino nitriles are important structural motifs in several pharmaceuticals such as Vildagliptin or Saxagliptin. Cyanidefree access to such nitriles is provided by a copper-catalyzed dehydration of oximes, which are readily available by condensation of chiral aldehydes resulting from the chiral pool with hydroxylamine. The application in a cascade process without the need for intermediate purification as well as a demonstrated scalability show the robustness of this methodology.
(S)-4/5-phenyl-2-(pyrrolidin-2-yl)thiazole TRPV1 antagonists as well as preparation and application thereof
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Paragraph 0050; 0124; 0126-0127, (2020/07/28)
The invention discloses (S)-4/5-phenyl-2-(pyrrolidin-2-yl)thiazole novel TRPV1 antagonists as well as a preparation method and application thereof, and particularly relates to compounds represented bya general formula (I) or a general formula (II) and a pharmaceutically acceptable salt thereof. The compound have a strong analgesic effect, the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC, almost no body temperature rise side effect exists, and the invention further relates to a preparation method of the compounds and pharmaceutical preparationscontaining the compounds.