The Article related to pyrimidine preparation gamma secretase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Bromo-2,4,6-trichloropyrimidine
On January 18, 2018, Bartels, Bjoern; Jakob-Roetne, Roland; Limberg, Anja; Neidhart, Werner; Ratni, Hasane; Reutlinger, Michael; Steiner, Sandra published a patent.Safety of 5-Bromo-2,4,6-trichloropyrimidine The title of the patent was Preparation of fused pyrimidine derivatives as γ-secretase inhibitors. And the patent contained the following:
The present invention relates to a compound of formula I wherein R1 is Ph, lower alkyl, C3-6-cycloalkyl, -CH2-C3-6-cycloalkyl or bridged C4-6-cycloalkyl, substituted by one, two or three halogen atoms, or by lower alkyl or lower alkyl substituted by halogen;R2 is a five or six membered heteroaryl group, selected from or wherein R6 is hydrogen, lower alkyl, halogen or lower alkoxy; and R7 is hydrogen, lower alkoxy or halogen; R3 is lower alkyl or lower alkyl substituted by hydroxy: R4 is hydrogen or lower alkyl; R5 is hydrogen or lower alkyl; n is 1 or 2; -( )n- is -CH2- or -CH2CH2- for n being 1 or 2; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer’s disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. Example compound II was prepared by amination of 2-chloro-7-(4-fluorophenyl)-N,5,5-trimethyl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-amine with (1R,5S,8S)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-amine. The invention compounds were evaluated for their γ-secretase inhibitory activity. From the assay, it was determined that compound II exhibited EC50 value of 14 nM. The experimental process involved the reaction of 5-Bromo-2,4,6-trichloropyrimidine(cas: 63931-21-5).Safety of 5-Bromo-2,4,6-trichloropyrimidine
The Article related to pyrimidine preparation gamma secretase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of 5-Bromo-2,4,6-trichloropyrimidine
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia