ChemicalBook CAS DataBase List FMoc-Val-Cit-PAB

FMoc-Val-Cit-PAB synthesis

11synthesis methods

Product Name:FMoc-Val-Cit-PAB
CAS Number:159858-22-7
Molecular formula:C33H39N5O6
Molecular Weight:601.69

Fmoc-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). The synthetic method of FMoc-Val-Cit-PAB is that：EEDQ was added in the mixtrue of Fmoc-Val-Cit-OH and PABOH in DCM and MeOH and stirred at room temperature for 14h. After the solution was purified to obtain Fmoc-Val-Cit-PAB as white solid.

159858-21-6
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623-04-1 Synthesis

623-04-1
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159858-22-7
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Yield:159858-22-7 98%

Reaction Conditions:

with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline in methanol;dichloromethane at 20; for 18.0833 h;

Steps:

1 Compound 8:

iV-Ethoxycarbonyl-2-ethoxy-l,2-dihydroquinoline (EEDQ, 1.99 g, 8.05 mmol) was added to a solution of p-aminobenzyl alcohol (0.99 g, 8.05 mmol) in dichloromethane (19 mL) and methanol (7.6 mL) at room temperature. After stirring for 5 min, Fmoc-Valine-Citrulline 7 (2.0 g, 4.03 mmol) was added in one portion and the resulting solution was stirred for 18 hours. Volatiles were removed in vacuo and the residue was triturated with ether (20 mL) and washed sequentially with ether (20 mL), ethyl acetate (20 mL), and ether (20 mL) to get title compound 8 (2.2 g, 98% yield) as a light yellowish solid. MS (ESI, pos.): calc’d for C33H39N5O6, 601.29; found 602.3 (M+H).

References:

WO2021/151031,2021,A1 Location in patent:Paragraph 00181; 00187-00188

1037794-22-1 Synthesis