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Asymmetric synthesis of α-aminophosphonic acids, I enantioselective synthesis of L-(1-aminoethyl)phosphonic acid by asymmetric catalytic hydrogenation ofN-[1-(dimethoxyphosphoryl)ethenyl]formamide

✍ Scribed by Schöllkopf, Ulrich ;Hoppe, Inga ;Thiele, Angelika


Book ID
102364518
Publisher
John Wiley and Sons
Year
1985
Tongue
English
Weight
275 KB
Volume
1985
Category
Article
ISSN
0947-3440

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✦ Synopsis


Abstract

The synthesis of N‐[bis(dimethoxyphosphoryl)methyl]formamide (7) from aminomethylene‐bis(phosphonic acid) (6) is described. 7 reacts with aldehydes in a Wittig‐Horner reaction to give N‐[1‐(dimethoxyphosphoryl)‐1‐alkenyl]formamides 3. From the parent compound 3a L‐(1‐amino‐ethyl)phosphonic acid (1) is obtained with e.e. ca. 76% via asymmetric catalytic hydrogenation using a rhodium catalyst in the presence of (+)‐DIOP.