147065-06-3Relevant articles and documents
Melphalan intermediate and preparation method thereof
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Paragraph 0043; 0058; 0063-0064; 0107; 0122; 0127-0128; 0171, (2019/08/02)
The invention discloses a Melphalan intermediate and a preparation method thereof. The Melphalan intermediate is prepared by acidifying a compound p-nitrobenzaldehyde under the action of methanol, a hydrochloric acid solvent, etc. The preparation method has a route with mild reaction conditions, is higher than an existing preparation method in yield, is economical and effective, and is suitable for large-scale industrial production. The synthesis route is as shown in the description.
Anthranilic acid based CCK1 receptor antagonists: Preliminary investigation on their second "touch point"
Varnavas, Antonio,Lassiani, Lucia,Valenta, Valentina,Mennuni, Laura,Makovec, Francesco,Hadjipavlou-Litina, Dimitra
, p. 563 - 581 (2007/10/03)
In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude greater than the lead and, as a general rule, it points out how the hypothesized receptorial pocket which accommodates the Phe residue allows much more structural modification than that interacting with the N-terminal group. Hence, the modification of the C-terminal pharmacophoric group of our lead VL-0395 can not only enhance the affinity of anthranilic acid derivatives but can modulate the selectivity for one CCK receptor subtype or afford mixed antagonists.