272775-65-2

Upstream product

• 50-00-0 formaldehyd 
• 41575-21-7 1,2-dichloro-4-(prop-1-en-2-yl)benzene 
• 18282-59-2 4-bromo-1,2-dichlorobenzene 
• 1034183-25-9 3-(3,4-Dichloro-phenyl)-but-3-enoic acid 
• 76334-36-6 3-bromobut-3-en-1-ol 
• 151169-75-4 3,4-dichlophenylboronic acid 
• 191673-76-4 methyl 3-(3,4-dichlorophenyl)-3-butenoate 

Downstream Products

• 191673-30-0 tert-Butyl-[3-(3,4-dichloro-phenyl)-but-3-enyloxy]-dimethyl-silane 
• 1013097-83-0 3-(3,4-dichlorophenyl)-3-buten-1-yl methanesulfonate 

Relevant academic research and scientific papers

NOVEL COMPOUNDS

The invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE

The present invention relates to novel compounds of formula (I)′, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R4 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4alkyl; R7 is hydrogen or C1-4alkyl; or is a group X, X1, X2 or X3; wherein X is (IV) X1 is (V) X2 is (VI) and X3 is (VII) R6 is hydrogen or C1-4alkyl; or is a group X or X1; R9 is C1-4alkyl; R10 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R13 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R15 is selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R16 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R17 is hydrogen or C1-4alkyl; R18 is selected from a group consisting of: halog

Formaldehyde Encapsulated in Zeolite: A Long-Lived, Highly Activated One-Carbon Electrophile to Carbonyl-Ene Reactions

Gaseous formaldehyde is extremely unstable and readily undergoes self-polymerization to a solid paraformaldehyde or disproportionation to methanol and formic acid in the presence of moisture. We disclose a simple method to stably store such a labile formaldehyde as a monomer in a nanoporous faujasite zeolite at 5 °C for at least 50 days without self-polymerization or disproportionation. The greater stability of formaldehyde encapsulated in zeolite was confirmed by 13C MAS NMR spectroscopy. Formaldehyde was not only stabilized within the zeolite cages but functioned as a powerful electrophile toward various olefins. Zeolite-encapsulated formaldehyde was proved to be a stable but highly reactive C1 reagent. Copyright

Practical carbonyl-ene reactions of α-methylstyrenes with paraformaldehyde promoted by a combined system of boron trifluoride and molecular sieves 4A

Matrix presented A combined system of boron trifluoride and molecular sieves is an efficient promoter for the carbonyl-ene reaction of a-methylsyrenes with paraformaldehyde. The coexistence of BF3-OEt2 and molecular sieves 4A is esse

An efficient synthesis of enantiomerically pure 2-[(2R)-arylmorpholin- 2-yl]ethanols, key intermediates of tachykinin receptor antagonist

We report herein an efficient and practical synthetic method for the preparation of enantiomerically pure 2[(2R)-arylmorpholin-2-yl]ethanols 1a- d, key intermediates of tachykinin receptor antagonist. Sharpless catalytic asymmetric dihydroxylation of 4a-d was employed to introduce the required absolute stereochemistry, and cyclization of 7a-d was accomplished by the Mitsunobu reaction.