917772-69-1Relevant articles and documents
Preparation method of 3-bromo-5-(propyn-1-yl)pyridine
-
, (2018/05/16)
The invention discloses a preparation method of 3-bromo-5-(propyn-1-yl)pyridine, comprising the steps of S1, subjecting N-methyl-N-methoxy-5-bromo-nicotinamide and ethyl carbon anion reagent to condensation reaction to generate (5-bromopyridine-3-yl)ethanone; S2, subjecting (5-bromopyridine-3-yl)ethanone and a chlorination reagent to reaction to obtain 3-bromo-5-(1,2-dichloropropene-1-yl)pyridine;S3, subjecting 3-bromo-5-(1,2-dichloropropene-1-yl)pyridine and a reducing agent to reaction to obtain 3-bromo-5-(propyn-1-yl)pyridine. The synthetic route is novel and has few steps; the target product can be prepared just via three steps of reaction; the yield is higher than 40%; using noble metal reagents is not required; the preparation method features mild reaction conditions and the like; materials used herein are easy to obtain and low in cost, and no special operating procedure is required; the requirement on equipment is low; the preparation method is suitable for industrial production.
COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS
-
Page/Page column 106; 107, (2016/11/17)
The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).
FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE
-
Paragraph 0252; 0253, (2013/08/28)
The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CRs