Abemaciclib synthetic routes

CAT#: 205911 | Name: Abemaciclib | CAS# 1231929-97-7

Purchases for research

Description:

Abemaciclib, also known as LY2835219, is orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.

Synthetic Routes

Abemaciclib - Synthetic Route 1

Abemaciclib - Synthetic Route 1

Synthetic Description

Reference:Chan ED. Combination of anti-human VEGFR2 antibody and abemaciclib for treatment of non-small cell lung cancer. WO 2015130540 (2015).

Abemaciclib - Synthetic Route 2

Abemaciclib - Synthetic Route 2

Synthetic Description

Reference:Frederick, MO.; Kjell, DP. A synthesis of abemaciclib utilizing a Leuckart-Wallach reaction. Tetrahedron Lett. 2015, 56(7); 949-951

Abemaciclib - Synthetic Route 3

Abemaciclib - Synthetic Route 3

Synthetic Description

Reference: Coates, DA.; Gelbert, LM.; Knobeloch, JM.; De dios Magana, A.; De Prado GA; Filadelfa del Prado Catalina, M.; Garcia Paredes, MC.; Martin de la Nava, EM.; Martin Ortega Finger, MD.; Martinez Perez, JA.; Mateo Herranz, AI.; Perez Martinez, C.; Sanchez Martinez, C. Preparation of benzimidazolylpyrimidinylaminopyridines as CDK4/6 protein kinase inhibitors. US 20100160340 (2010).

Abemaciclib - Synthetic Route 4

Abemaciclib - Synthetic Route 4

Synthetic Reference

Qi, Yuxin; Liu, Yuesheng; Zhu, Chengchen; Zhang, Mingfeng; Wang, Tao. Preparation of abemaciclib intermediate and abemaciclib. Assignee Xinfa Pharmaceutical Co., Ltd. CN 110218189. 2019.

Abemaciclib - Synthetic Route 5

Abemaciclib - Synthetic Route 5

Synthetic Reference

Jetti, Ramakoteswara Rao; Indukuri, Anjaneyaraju; Bommareddy, Aggi Ramireddy; Srinivasarao, Attanti Veera Venkata; Jebaraj, Rathinapandian; Chandupatla, Shivakumar; Batharaju, Ramesh; Kunamneni, Sunil. Crystalline polymorphs of abemaciclib. Assignee Mylan Laboratories Limited.WO 2019102492. 2019.

Abemaciclib - Synthetic Route 6

Abemaciclib - Synthetic Route 6

Synthetic Reference

Albrecht, Wolfgang; Rabe, Sebastian. Abemaciclib form IV. Assignee Ratiopharm GmbH. WO 2017108781. 2017.