- Azabicyclic amino acids by stereoselective dearomatizing cyclization of the enolates of N-nicotinoyl glycine derivatives
-
On activation by pyridine N-acylation, enolates of N-nicotinoyl and N-isonicotinoyl glycine and alanine derivatives cyclize to yield 6,5-azabicyclic or 6,4-azaspirocyclic lactams. With an N-α-methyl-p-methoxybenzyl group the cyclization is diastereoselect
- Arnott, Gareth,Clayden, Jonathan,Hamilton, Stuart D.
-
p. 5325 - 5328
(2007/10/03)
-
- Reactions of Benzotriazole with Formaldehyde and Aliphatic Primary Amines: Selective Formation of 1:1:1, of 2:2:1, and of 2:3:2 Adducts and a Study of their Reactions with Nucleophiles
-
Benzotriazole (BtH) reacts easily with aliphatic primary amines and formaldehyde in aqueous media to give one or more of three types of product: (i) (BtCCH2)2NR (5), (ii) (BtCH2NR)2CH2 (6), and/or (iii) BtCH2NHR (7).The product formed depends on the molar
- Katritzky, Alan R.,Pilarski, Boguslaw,Urogdi, Laszlo
-
p. 541 - 547
(2007/10/02)
-
- O,O-Dialkyl-N-(benzyl or t-butyl)-N-cyanomethyl aminomethylphosphonates
-
A method of preparing N-phosphonomethylglycine comprising reacting a compound having the structural formula wherein R is tertiary butyl or STR1 wherein Ar is an aromatic group, R1 and R2 are independently hydrogen, C1 -C10 alkyl or an aromatic group, with formaldehyde and a phosphite to form a tertiary amine and hydrolyzing the tertiary amine in the presence of hydrochloric, hydrobromic, or hydriodic acid to yield N-phosphonomethylglycine.
- -
-
-
- β Adrenergic blocking agents. Nitrogen heteroaryl substituted 2 propanolamines and ethanolamines
-
A series of some 20 novel 2 propanolamines of type I was prepared by reaction of Het CH2Li with the properly substituted aminoacetonitrile, followed by hydrolysis and reduction. The most potent β adrenergic blocking activity was found in the phenanthridine, quinoline, and isoquinoline series, the phenanthridine being almost 10 times as active as propranolol. Some ethanolamine homologs of the phenanthridine and quinoline series were prepared for comparison, the former being toxic, the latter somewhat more active than the corresponding 2 propanolamine.
- Meyer,Stratton,Hastings,Corey
-
p. 1113 - 1116
(2007/10/05)
-