20989-42-8Relevant articles and documents
Metal-Free Selective Modification of Secondary Amides: Application in Late-Stage Diversification of Peptides
Adebomi, Victor,Sriram, Mahesh,Streety, Xavier,Raj, Monika
supporting information, p. 6189 - 6193 (2021/08/01)
Here we solve a long-standing challenge of the site-selective modification of secondary amides and present a simple two-step, metal-free approach to selectively modify a particular secondary amide in molecules containing multiple primary and secondary amides. Density functional theory (DFT) provides insight into the activation of C-N bonds. This study encompasses distinct chemical advances for late-stage modification of peptides thus harnessing the amides for the incorporation of various functional groups into natural and synthetic molecules.
Synthesis method of ramipril key intermediate
-
Paragraph 0045; 0046; 0060; 0061; 0073; 0074, (2017/08/29)
The invention discloses a synthesis method of a ramipril key intermediate. The ramipril key intermediate is 2-azabicyalo [3.3.0] octane-3-carboxylic acid hydrochloride. The 2-azabicyalo [3.3.0] octane-3-carboxylic acid hydrochloride is obtained through sequential dehydration cyclization, formaldehyde condensation, hydrolysis, removal, Michael addition, cyclization and palladium-carbon catalytic hydrogenation reduction of N-benzoyl-glycine as a raw material. According to the synthesis method of the ramipril key intermediate, the required raw material and reagent are cheap and available, the yield is relatively high, the operation is simple, the cost is low and the method is suitable for industrial production.
The rapid synthesis of oxazolines and their heterogeneous oxidation to oxazoles under flow conditions
Gl?ckner, Steffen,Tran, Duc N.,Ingham, Richard J.,Fenner, Sabine,Wilson, Zoe E.,Battilocchio, Claudio,Ley, Steven V.
supporting information, p. 207 - 214 (2015/02/02)
A rapid flow synthesis of oxazolines and their oxidation to the corresponding oxazoles is reported. The oxazolines are prepared at room temperature in a stereospecific manner, with inversion of stereochemistry, from β-hydroxy amides using Deoxo-Fluor. The