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ChemicalBook CAS DataBase List MC-Val-Cit-PAB
159857-80-4

MC-Val-Cit-PAB synthesis

11synthesis methods
MC-VAL-CIT-PAB is a cathepsin-cleavable ADC bridge for the preparation of antibody-drug conjugates. It was prepared from vc-PABOH and MC-OSu by stirring in NMP for 24h at 40℃.
55750-63-5 Synthesis
N-Succinimidyl 6-maleimidohexanoate

55750-63-5
326 suppliers
$6.00/50mg

159857-79-1 Synthesis
Val-cit-PAB-OH

159857-79-1
229 suppliers
$32.00/5mg

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Yield:159857-80-4 100%

Reaction Conditions:

in 1-methyl-pyrrolidin-2-one for 24 h;Heating;

Steps:

7 Example 7. Synthesis of mc-vc-PABOH
vc-PABOH 205 mg (0.54 mmol) and MC-OSu 184 mg (1.1 eq) were added to 10 ml of NMP.The reaction was stirred for 24 h under warming. After completion of the reaction, the mixture was concentrated under reduced pressure at 40° C., and 20 ml of methyl tert-butyl ether was added to the resulting oil.Crystallization. It was filtered and the cake was washed with methyl tert-butyl ether to give 310 mg of product in 100% yield.

References:

Sichuan Bai Li Pharmaceutical Co., Ltd.;Zhu Yi;Wang Yiqian;Zhuo Shi;Li Jie;Chen Lan;Wan Weili;Yu Yongguo CN107789630, 2018, A Location in patent:Paragraph 0079; 0080; 0081

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