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ChemicalBook CAS DataBase List CAL-101
870281-82-6

CAL-101 synthesis

5synthesis methods
Idelalisib, also known as CAL-101, is a PI3K-delta inhibitor with potential immunomodulating and antineoplastic activities. CAL-101 inhibits the production of the second messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3), preventing the activation of the PI3K signaling pathway and thus inhibiting tumor cell proliferation, motility, and survival. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in hematopoietic lineages. The targeted inhibition of PI3K-delta is designed to preserve PI3K signaling in normal, non-neoplastic cells. CAL-101 has [EC(50)] = 8nM.
Synthetic Routes
  • ROUTE 1
  • 202112073231361669.jpg

    Cai, Duo-Te; Zhang, Yue-Bin; Chen, Ken; Xiong, Qi-Xing; Luo, Wen-Juan; Gao, Zhi-Gang. Synthesis and evaluation of a novel heterocyclic compound against pediatric hepatoblastoma cells. Latin American Journal of Pharmacy. Volume 36. Issue 10. Pages 2022-2027. Journal. (2017).

  • ROUTE 2
  • 202112073264997456.jpg

    Liu, Jian; Huang, Yu; Chang, Xiao-hui; Liu, Xiang-kui; Jiang, Hui-juan; Zhu, Xue-yan. A Novel Method of Preparing (S)?-?5-?Fluoro-?3-?phenyl-?2-?[1-?(9H-?purin-?6-?ylamino)?propyl]?-?3H-?quinazolin-?4-?one. Organic Preparations and Procedures International. Volume 48. Issue 4. Pages 337-341. Journal; Online Computer File. (2016).

  • ROUTE 3
  • 202112072073420693.jpg

  • ROUTE 4
  • 202112076188334785.jpg

    Kompella, Amala; Rachakonda, Sreenivas; Gampa, Venugopala Krishna; Kusumba, Subhash; Konakanchi, Durga Prasad; Muddasani, Pulla Reddy; Nannapaneni, Venkaiah Chowdary. Process for the preparation of amorphous idelalisib. Assignee?Natco Pharma Limited, India. WO2018198131. (2018).

  • ROUTE 5
  • 202112078214465325.jpg

    Thennati, Rajamannar; Dwivedi, Shriprakash Dhar; Jadav, Kanaksinh Jesingbhai; Patel, Vimeshkumar Maganlal; Joshi, Krunalkumar Chetanbhai. Process for the preparation of Idelalisib. Assignee?Sun Pharmaceutical Industries Limited, India. WO?2017221272. (2017).

  • ROUTE 6
  • 202112075582192154.jpg

    Oruganti, Srinivas; Sen, Saikat; Dahanukar, Vilas Hareshwar. Processes for preparation of idelalisib and intermediates thereof. Assignee?Dr. Reddy\'s Laboratories Limited, India. IN?2014CH06844. (2016).

202112073231361669.jpg

Cai, Duo-Te; Zhang, Yue-Bin; Chen, Ken; Xiong, Qi-Xing; Luo, Wen-Juan; Gao, Zhi-Gang. Synthesis and evaluation of a novel heterocyclic compound against pediatric hepatoblastoma cells. Latin American Journal of Pharmacy. Volume 36. Issue 10. Pages 2022-2027. Journal. (2017).

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Yield:870281-82-6 3.1 g

Reaction Conditions:

with triethylamine in tert-butyl alcohol at 30 - 85; for 24 h;Concentration;Reagent/catalyst;

Steps:

28 Preparation of ldelalisib

(S)-2-(1 -aminopropyl)-5-fluoro-3-phenylquinazolin-4(3H)-one prepared in example 26 (4.2 g) and t-Butanol (21 mL) were charged into a 100 mL round bottom flask. Triethylamine (3.91 mL) and 6-Chloropurine (2.5 g) were added at 30 00. The resultant reaction mixture was heated to85°C and stirred for 24 hours. The reaction mixture was evaporated completely under reduced pressure at 40°C. The resultant residue was diluted with water (100 mL) and stirred for 30 minutes. The precipitate was filtered and the solid was washed with water (30 mL) and n-Hexane (50 mL) and dried for 1 hour under vacuum. The crude was purified by chromatographyusing Si02 (1 00:200) (solvent MeOH: DCM: TEA:: 5: 94: 1). The eluted fractions were evaporated completely under vacuum. The isolated product was diluted in dichloromethane (100 mL) and the organic layer was washed with brine solution (2x25 mL). The organic layer dried over sodium sulphate (10 g) and evaporated under reduced pressure to yield 3.1 g of Idelalisib as pale yellow solid.Purity: 97.87% by HPLC; chiral purity: 98.77% by H PLC

References:

WO2016/108206,2016,A2 Location in patent:Page/Page column 49; 50

CAL-101 Related Search:

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