- Guanidine Synthesis: Use of Amidines as Guanylating Agents
-
The use of amidines for the tandem or one-pot synthesis of guanidines is reported. Guanidines are obtained by oxidative rearrangement of readily available and stable amidines into carbodiimides, followed by in situ reaction with amines. The protocol can be executed under mild reaction conditions (30°C), in a green solvent (dimethyl carbonate). The amine scope is broad, including sterically hindered, oxidation-sensitive and chiral amines. Examples for the synthesis of both acyclic and cyclic guanidines are provided. 2-Propoxyphenyl iodide (2-PrOPhI) by-product, generated from the oxidant [N-(p-toluenesulfonyl)imino](2-propoxyphenyl)iodinane (2-PrOPhINTs), can be isolated in high yields making regeneration of the hypervalent iodine reagent possible. The utility and greenness of the synthetic method versus the state-of-the-art is demonstrated by a new route towards the antihypertensive drug Pinacidil. The process mass intensity (PMI) of the new route is only 24% of the classical one.
- Baeten, Mattijs,Maes, Bert U. W.
-
supporting information
p. 826 - 833
(2016/03/12)
-
- Novel heterocycles 3
-
The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
- -
-
-
- Pyrimidine derivatives
-
This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): and stereoisomers thereof, wherein, R1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by a
- -
-
-
- Insecticidally and acaricidally active pyrimidine esters and intermediates therefor
-
This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): STR1 and stereoisomers thereof, wherein R1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally s
- -
-
-
- 2,6-disubstituted-5-cyano-4-pyrimidinyloxyacetic acid aldose reductase inhibitors
-
Disclosed herein are 2,6-disubstituted-5-cyano-4-pyrimidinyloxyacetic acids and pharmaceutically acceptable salts thereof and methods of their preparation. The compounds are new aldose reductase inhibitors useful for the treatment or prevention of diabeti
- -
-
-
- Pyrimidine derivatives
-
A compound of formula: STR1 wherein R1 represents hydrogen or halogen, R2 represents an α-branched alkyl or a cycloalkyl group containing from 3 to 6 carbon atoms, Q represents hydroxy, halo, alkoxy of up to 6 carbon atoms or a group --OR where R represents the residue of an alcohol of formula ROH which forms an insecticidal ester when combined with crysanthemic acid, or 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylic acid, or 3-(2-chloro-3,3,3-trifluoroprop-1-en-1-yl)-2,2-dimethylcyclopropane carboxylic acid. The compounds are useful for combating insect and acarime pests.
- -
-
-
- Pyrimidine substituted-2,2-dimethylcyclopropane carboxylates useful for combating insect and acarine pests at a locus
-
A compound of formula: STR1 wherein R2 represents an α-branched alkyl group containing from 3 to 6 carbon atoms, and R represents either (a) hydroxy, halo or alkoxy of up to six carbon atoms, or (b) the group --OR1 where R1 is the residue of an alcohol of formula R1 OH which forms an insecticidal ester with chrysanthemic acid, permethrin acid or cyhalothrin acid. The compounds have insecticidal and acaricidal properties.
- -
-
-
