252008-94-9

Upstream product

• 115962-35-1 (3S)-2-tert-butoxycarbonyl-1,2,3,4-tetrahydroisoquinole-3-carboxylic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 24424-99-5 di-tert-butyl dicarbonate 
• 74163-81-8 L-Tic-OH 
• 74-88-4 methyl iodide 

Downstream Products

• 79815-19-3 methyl (3S)-1,2,3,4-tetrahydro-3-isoquinolinecarboxylate 
• 929207-33-0 methyl (3S)-N-phenylcarbamoyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylate 
• 393837-14-4 methyl (3S)-2-[(benzylamino)carbonyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxylate 
• 183958-71-6 tert-butyl (3S)-3-(hydroxymethyl)-3,4-dihydroisoquinoline-2(1H)-carboxylate 

Relevant academic research and scientific papers

PRMT5 INHIBITORS

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

PRMT5 INHIBITORS

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.

PYRAZOLO [1, 5 -A] PYRIMIDINES AS ANTIVIRAL AGENTS

The invention provides compounds of Formula I or Formula II: (I), (II) or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPARδ agonists

Small molecule isoindoline and tetrahydroisoquinoline derivatives have been identified as selective agonists of human peroxisome proliferator-activated receptor δ (PPARδ. Compound 18 demonstrated efficacy in a biomarker for increased fatty acid oxidation,

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 2

Herein is described a new class of selective σ1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 1a has high affinity (IC50 = 16 nM) for σ1 receptor and is selective in a large panel of therapeutic targets. This study presents structural changes on the side chain of the Tic-hydantoin core. Analogs of higher affinity could be identified (IC50 ≈ 2-3 nM).

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective σ1 ligands. Part 1

Herein is described a new class of selective σ1 ligands consisting of tetrahydroisoquinoline-hydantoin (Tic-hydantoin) derivatives. Compound 3a has high affinity (IC50 = 16 nM) for the σ1 receptor and is selective in a large panel of therapeutic targets. This first study presents structural changes around the Tic-hydantoin core, leading to a Tic-hydantoin analogue with a higher σ1 affinity (IC50 ≈ 1 nM).

Optimized synthesis of tetrahydroisoquinoline-hydantoins

Several methods have been developed and compared for the solution synthesis of tetrahydroisoquinoline-hydantoin derivatives. The best yields were obtained when the imidazolidine-2,4-dione ring was synthesized in two steps: (1) reaction of Tic-OH with the appropriate amine and (2) cyclization with 1,1′-carbonyldiimidazole.

Convenient synthesis of tetrahydroisoquinoline-hydantoins

NaOH/MeOH or DIEA/CH2Cl2 were convenient conditions for the synthesis in solution phase of hydantoins derived from Tic-OH and isocyanates.