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ChemicalBook CAS DataBase List Val-cit-PAB-OH
159857-79-1

Val-cit-PAB-OH synthesis

11synthesis methods
Val-cit-PAB-OH acts as a reagent in the preparation of cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy, preparation of monomethylvaline derivative conjugates with ligands and antibodies for cancer treatment. It was prepared from FMoc-Val-Cit-PAB with diethyl amine by stirring in DMF for 16 h at room temperature.
159858-22-7 Synthesis
FMoc-Val-Cit-PAB

159858-22-7
217 suppliers
$14.00/25MG

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Yield:159857-79-1 100%

Reaction Conditions:

with diethylamine in N,N-dimethyl-formamide for 24 h;

Steps:

5 Synthesis of (S)-2-((S)-2-amino-3-methylbutanamido)-N-(4-(hydroxymethyl)phenyl)- 5-ureidopentanamide 6:
Compound 5 (4.0 g, 6.65 mmol) was dissolved in DMF (80 mL) and diethyl amine (14 mL) was added. The reaction mixture was stirred for 24 hours. [0560] The reaction mixture was evaporated to dryness to give a residue. The residue was titurated with dichloromethane to give a light brown solid in 2.5 g for a quantitative yield. The compound was used in the next step without further purification.

References:

IL-2RX, INC.;SOARES, Luis R.B.;HURT, Clarence Ray WO2020/14541, 2020, A2 Location in patent:Paragraph 0546; 0551; 0559-0560

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