Active  name:	Capivasertib
Brand name:	Truqap
Innovator name	ASTRAZENECA PHARMACEUTICAL LTD
Approval Date:	Nov 16, 2023
Therapeutic activity:	Capivasertib, in combination with fulvestrant, is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer.
Route of adminstration	Tablet, oral
Structure
Chemical name	4-amino-N-[(1S)-1-(4- chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinecarboxamide
CAS	11143532-39-1
Dosage	160 & 200 mg
MDD	320 mg
Molecular weight& molecular formuale	428.92 g/mol & C21H25ClN6O2
OB patents	US 8101623 B2; US9487525 B2; US10059714B2;
Polymorhic patent	US9487525 B2;
NCE	11/16/2028
Solubility data	Freely soluble in water when pH below 1.2 and practically insoluble pH above 6.8.
Hygroscopicity	Not hygroscopic
Pubchem CID	25227436
Drugbank	DB12218
Chemspider	28189073

Patent No	Patent Expiration	Drug Substance	Drug Product	Patent Use Code	Delist Requested	Submission Date
8101623	03/10/2030	DS	DP	U-3762		12/13/2023
8809336	10/25/2025			U-3762		12/13/2023
9006430	10/25/2025		DP			12/13/2023
9487525	04/16/2033	DS	DP			12/13/2023
10039766	04/16/2033			U-3762		12/13/2023
10059714	10/10/2028	DS	DP			12/13/2023
10654855	10/10/2028			U-3762		12/13/2023
11760760	10/10/2028			U-3762		12/13/2023

Route of synthesis:

Scheme-1:

US 8101623B2 reported the synthesis of Capivasertib from 4-chloro phenyl alaninol.

Scheme-2:

US 8101623B2 reported the synthesis of Capivasertib from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine  and 4-(tert-butoxycarbonylamino)piperidine-4-carboxylic acid.

Scheme-3:

US 8101623B2 reported the synthesis of Capivasertib from 4-chloro-7H-pyrrolo[2,3-d]pyrimidine  and 4-(tert-butoxycarbonylamino)piperidine-4-carboxylic acid.

References:

ournal of Medicinal Chemistry

Cite this: J. Med. Chem. 2013, 56, 5, 2059–2073

https://doi.org/10.1021/jm301762v

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