- Direct Exploitation of the Ethynyl Moiety in Calcium Carbide Through Sealed Ball Milling
-
Ball milling of calcium carbide (CaC2) enables the reaction of its ethynyl moiety with organic electrophiles. This was realized simply by co-milling CaC2 with organic substrates in a sealed jar without the need for an additive or a catalyst. Various ketones including those bearing α-hydrogens were ethynylated in good yields at short reaction times. Aryl halides are also amenable substrates for this protocol as they furnish aryl ethynes through a benzyne intermediate. This method offers a practical and cheap alternative to the established procedures for introducing ethynyl functionalities.
- Hosseini, Abolfazl,Schreiner, Peter R.
-
p. 4339 - 4346
(2020/07/04)
-
- Alkyl group-tagged ruthenium indenylidene complexes: Synthesis, characterization and metathesis activity
-
We report on the synthesis of ruthenium indenylidene catalysts [RuCl2(3-R-1-indenylidene)(PCy3)2 in which R is iso-propyl (7a), tert-butyl (7b) or cyclohexyl (7c)]. The obtained alkyl tagged indenylidene catalysts were ana
- Yu, Baoyi,Hamad, Fatma B.,Leus, Karen,Lyapkov, Alex A.,Van Hecke, Kristof,Verpoort, Francis
-
p. 148 - 154
(2015/06/22)
-
- CATALYST COMPLEXES WITH CARBENE LIGAND AND METHOD FOR MAKING SAME AND USE IN METATHESIS REACTION
-
This invention relates to catalyst compounds and the synthesis and applications useful in olefin metathesis reactions. The catalyst compounds of the invention are represented by the formula (I): wherein M is a Group 8 metal; X1 and X2/sup
- -
-
Page/Page column 29
(2014/07/23)
-
- 1-Aryl-1-hydroxy-1-substituted-3-(4-substituted-1-piperazinyl)-2-propanones and their use in treatment of neurogenic bladder disorders
-
Compounds are disclosed having the formula (I): in which R1is a C1 to C12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons; R2is hydrogen, phenyl, phenyl singly or multiply substituted with halogen, hydroxy, lower alkoxy, methylene dioxy, nitro, lower alkyl or trifluoromethyl, lower alkyl, said alkyl being branched chain or straight, saturated, unsaturated, or cyclic and substituted or unsubstituted, said substituents being selected from thienyl, pyrrolyl, pyridyl, furanyl, hydroxy, lower alkoxy, or acetoxyalkyl wherein the alkyl group has 1 to 3 carbons, phenyl, phenyl substituted with halogen, hydroxy, lower alkoxy, lower alkyl, nitro, methylene dioxy or trifluoromethyl, Phis phenyl or phenyl para-substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl; and the pharmaceutically acceptable nontoxic salts thereof. The preparation of the compounds, pharmaceutical compositions containing them and their use in the treatment of neurogenic bladder disorder are also enclosed.
- -
-
-
- Analogues of oxybutynin. Synthesis and antimuscarinic and bladder activity of some substituted 7-amino-1-hydroxy-5-heptyn-2-ones and related compounds
-
Oxybutynin chloride [4-(diethylamino)-2-butynyl α-cyclohexyl-α-hydroxybenzeneacetate hydrochloride, Ditropan] is widely used for the relief of symptoms in neurogenic bladder. This is a result of its combined anticholinergic, antispasmodic, and local anesthetic activities. In a study directed toward development of agents possessing the beneficial properties of oxybutynin, but having a longer duration of action, a series of metabolically more stable keto analogues of the parent ester, i.e. substituted 7-amino-1-hydroxy-5-heptyn-2-ones along with some analogues and derivatives, was prepared and evaluated for in vitro and in vivo antimuscarinic action in guinea pig preparations. Several members of the series were potent antimuscarinics having a longer duration of activity than that of oxybutynin in a guinea pig cystometrogram model. On the basis of its in vitro and in vivo antimuscarinic activity, coupled with a 5-fold greater duration of action than that of oxybutynin, 1-cyclobutyl-7-(dimethylamino)-1-hydroxy-1-phenyl-5-heptyn-2-one (14b) was selected for clinical evaluation.
- Carter,Noronha-Blob,Audia,Dupont,McPherson,Natalie Jr.,Rzeszotarski,Spagnuolo,Waid,Kaiser
-
p. 3065 - 3074
(2007/10/02)
-
- 1-aryl-1-hydroxy-1-substituted-3-(4-substituted-1-piperazinyl)-2-propanones and their use in treatment of neurogenic bladder disorders
-
Compounds are disclosed having the formula: STR1 in which R1 is a C1 l to C12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons; R2 is hydrogen, phenyl, phenyl singly or multiply substituted with halogen, hydroxy, lower alkoxy, methylene dioxy, nitro, lower alkyl or trifluoromethyl, lower alkyl, said alkyl being branched chain or straight, saturated, unsaturated, or cyclic and substituted or unsubstituted, said substituents being selected from thienyl, pyrrolyl, pyridyl, furanyl, hydroxy, lower alkoxy, or acetoxyalkyl wherein the alkyl group has 1 to 3 carbons, phenyl, phenyl substituted with halogen, hydroxy, lower alkoxy, lower alkyl, nitro, methylene dioxy or trifluoromethyl, Ph is phenyl or phenyl para-substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl; and the pharmaceutically acceptable nontoxic salts thereof. Pharmaceutical compositions containing the compounds and methods for the treatment of neurogenic bladder disorders are also disclosed. In the preferred compound Ph is phenyl, R1 is cyclobutyl and R2 is benzyl.
- -
-
-
- 1,7-substituted heptyn-2-ones and use
-
1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C1 to C7 alkyl, C3 to C6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidy
- -
-
-