LEE011 (succinate)

Base Information

• Chemical Name: LEE011 (succinate)
• CAS No.: 1374639-75-4
• Molecular Formula: C23H30N8O.C4H6O4
• Molecular Weight: 552.62534
• Mol file: 1374639-75-4.mol

Synonyms:LEE011 (succinate);7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate;LEE-011 succinate salt, Ribociclib succinate salt

Chemical Property of LEE011 (succinate)

Chemical Property:

• PSA: 165.81000
• LogP: 3.19900
• Storage Temp.: Refrigerator
• Solubility.: DMSO (Slightly), Methanol (Slightly)

Purity/Quality:

97% ^*data from raw suppliers

LEE011Succinate ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

Useful:

• Uses: LEE011 is an orally bioavailable and highly specific CDK4/6 (cyclin-dependent kinase 4/6) inhibitor. LEE011 in combination with LGX818 (a V600E BRAF specific inhibitor) or BYL719 (a PIK3CA specific inhibitor) leads to robust anti-tumor activity in melanoma and breast cancer tumor models.

Technology Process of LEE011 (succinate)

There total 32 articles about LEE011 (succinate) which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 97.1%

succinic acid (110-15-6) + (7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide) (1211441-98-3) → 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide succinate salt (1374639-75-4)

Guidance literature:

In tetrahydrofuran; at 25 - 70 ℃; Solvent; Temperature;

Reference yield: 94.9%

succinic acid (110-15-6) + (7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide) (1211441-98-3) → 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate (1374639-75-4)

Guidance literature:

In isopropyl alcohol; at 27 - 83 ℃; Inert atmosphere;

Reference yield: 90.0%

succinic acid (110-15-6) + N,N‐dimethyl‐7‐cyclopentyl‐2‐{[5‐(4-tert-butoxycarbonylpiperazin‐1‐yl)pyridin‐2‐yl]amino}‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxamide (1374639-78-7) → 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide succinate salt (1374639-75-4)

Guidance literature:

N,N‐dimethyl‐7‐cyclopentyl‐2‐{[5‐(4-tert-butoxycarbonylpiperazin‐1‐yl)pyridin‐2‐yl]amino}‐7H‐pyrrolo[2,3‐d]pyrimidine‐6‐carboxamide; With toluene-4-sulfonic acid; In isopropyl alcohol; at 60 - 65 ℃;

succinic acid; In methanol; at 60 - 80 ℃; for 2h;

upstream raw materials:

Cyclopentamine

succinic acid

(7-cyclopentyl-Ν,Ν-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo [2,3-d]pyrimidine-6-carboxamide)

tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate