Synthesis of Hexamine Ligands by Using Trityl as an N-Blocking Group
摘要:
The amino-groups of diethylenetriamine were regioselectively protected by trityl groups and then reacted with dihalogenated alkylane to give the terminal N-blocked hexamine derivatives, from which a series of hexamine ligands (5(a-f)) were obtained by removing the trityl groups with 5.0 M HCl solution. Alternatively, the hexamine ligands could be also prepared via amidation and reduction reactions. The synthetic routes described here are mild, efficient and easy to handle.
[EN] TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER<br/>[FR] PRODUITS RADIOPHARMACEUTIQUES CIBLÉS POUR LE DIAGNOSTIC ET LE TRAITEMENT DU CANCER DE LA PROSTATE
申请人:BAYER AS
公开号:WO2021013978A1
公开(公告)日:2021-01-28
A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.
The novel fluoroussupport Hfb (hexakisfluorous chain-type butanoyl) was easily prepared. The Hfb group was readily introduced into the anomeric hydroxyl group of a carbohydrate, and was recyclable after cleavage. The use of the Hfb group was applicable for the rapid oligosaccharidesynthesis in which the synthetic intermediates could be purified using fluorous and normal organic solvents. Each synthetic
Synthesis of Hexamine Ligands by Using Trityl as an N-Blocking Group
作者:Erle Zang、Peter J. Sadler
DOI:10.1080/00397919708004172
日期:1997.9
The amino-groups of diethylenetriamine were regioselectively protected by trityl groups and then reacted with dihalogenated alkylane to give the terminal N-blocked hexamine derivatives, from which a series of hexamine ligands (5(a-f)) were obtained by removing the trityl groups with 5.0 M HCl solution. Alternatively, the hexamine ligands could be also prepared via amidation and reduction reactions. The synthetic routes described here are mild, efficient and easy to handle.