Inducers of apoptosis for the treatment of cancer and immune and autoimmune diseases
A therapeutic agent, a technology for small cell lung cancer, applied in the directions of organic active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as cytotoxicity and weak binding
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
preparation example Construction
[1294] After preparation as described in Scheme 1, compounds of formula (6) can be combined with boronic acids of formula (8) under Suzuki, Stille, or Negishi coupling conditions known to those skilled in the art and readily available in the literature. boronate equivalent (boronate equivalent)) or an organotin or organozinc halide compound of formula (8a) (wherein Y 1 , L 1 , and Y 2 Reaction as described herein with M being tributyltin or zinc halide) affords compounds of formula (I). Alternatively, compounds of formula (7), which can be prepared as described in Scheme 1 from compounds of formula (6), can be combined with formula (6) under Suzuki coupling conditions known to those skilled in the art and readily available in the literature (9) compound (wherein X 1 is triflate or halide, and Y 1 , L 1 , and Y 2 as described herein) to give compounds of formula (I).
[1295]
[1296] As shown in Scheme 3, where R x1 is hydrogen or Y as described herein 1 The formul...
Embodiment 1
[1310] 6-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl]-3-(1-benzyl-1H- Pyrazol-4-yl)pyridine-2-carboxylic acid
Embodiment 1A
[1312] 8-(Benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinoline-2(1H)-carboxylic acid tert-butyl ester
[1313] To 2-(tert-butoxycarbonyl)-1,2,3,4-tetrahydroisoquinoline-8-carboxylic acid (6.8 g) and benzo[ d ] Thiazol-2-amine (5.52 g) in dichloromethane (80 mL) solution, add 1-ethyl-3-[3-(dimethylamino) propyl]-carbodiimide hydrochloride ( 9.4 g) and 4-dimethylaminopyridine (6 g). The mixture was stirred overnight at room temperature. The reaction mixture was diluted with dichloromethane (400 mL), washed with 5% aqueous HCl, water and brine, and washed with Na 2 SO 4 dry. The mixture was filtered and the filtrate was concentrated under reduced pressure to afford the title compound.
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More