- Preparation method of varenicline key intermediate
-
The invention discloses a preparation method of a varenicline key intermediate. A target compound is prepared from indanone by the six steps of halogenation, cyanidation, hydrolysis, closed-loop reaction, reduction and hydrochloride formation. The preparation method has the advantages of easy availability of raw materials, mild reaction conditions, simple process, high yield, low cost, low environmental pollution and good utilization value in industrial production.
- -
-
Paragraph 0099-0113
(2019/04/04)
-
- Synthesis of 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine via oxidative cleavage and reductive amination strategies
-
Preparations of 2,3,4,5-tetrahydro-1,5-methano-1H-3-benzazepine (5) from benzonorbornadiene (1) by oxidative cleavage and reductive amination sequences were investigated. Osmium-mediated dihydroxylation of 1 followed by NaIO 4 cleavage, reductive amination and debenzylation provides 5 in 64-73% yield overall in three operations. A tandem ozonolysis-reductive amination procedure gives 5 as the tosylate salt from benzonorbornadiene with no isolation of intermediates in 28% yield.
- Brooks, Paige R.,Caron, Stephane,Coe, Jotham W.,Ng, Karl K.,Singer, Robert A.,Vazquez, Enrique,Vetelino, Michael G.,Watson Jr., Harry H.,Whritenour, David C.,Wirtz, Michael C.
-
p. 1755 - 1758
(2007/10/03)
-
- Nicontinic acetylcholine receptor antagonists in the treatment of restless legs syndrome
-
This invention relates to the use of nicotinic acetylcholine receptor agonists for the treatment of restless legs syndrome (RLS). The invention further relates to the use of a nicotinic acetylcholine receptor agonist in the manufacture of a medicament for the treatment of RLS. The present invention also relates to a pharmaceutical composition for the treatment of RLS containing a nicotinic acetylcholine receptor agonist.
- -
-
-