Chidamide

CAS No.: 743420-02-2

Chemical Name:: Chidamide

Synonyms: CS-1764;Chidamide;HBI-8000);HDAC-IN-7;Chidamide D4;Chidamide(CS055;chidamide analog;Chidamide impurity;Chidamide USP/EP/BP;Tucidinostat (Chidamide)

CBNumber:: CB42590631

Molecular Formula:: C22H19FN4O2

Molecular Weight:: 390.41

MOL File:: 743420-02-2.mol

MSDS File:: SDS

Modify Date:: 2023/5/18 11:31:21

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Chidamide Properties

Melting point	>145°C (dec.)
Boiling point	600.2±55.0 °C(Predicted)
Density	1.336±0.06 g/cm3(Predicted)
storage temp.	2-8°C(protect from light)
solubility	DMSO (Slightly), Methanol (Slightly, Sonicated)
form	Solid
pka	12.30±0.70(Predicted)
color	Off-White to Pale Beige

Chidamide Chemical Properties,Uses,Production

Description

Chidamide (Epidaza®), a class I HDAC inhibitor, was discovered and developed by ChipScreen and approved by the CFDA in December 2014 for the treatment of recurrent of refractory peripheral T-cell lymphoma. Chidamide, also known as CS055 and HBI- 8000, is an orally bioavailable benzamide type inhibitor of HDAC isoenzymes class I 1–3, as well as class IIb 10, with potential antineoplastic activity. It selectively binds to and inhibits HDAC, leading to an increase in acetylation levels of histone protein H3.74 This agent also inhibits the expression of signaling kinases in the PI3K/ Akt and MAPK/Ras pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. Currently, phases I and II clinical trials are underway for the treatment of non-small cell lung cancer and for the treatment of breast cancer, respectively.

Uses

De-5-fluoro 4-Fluorochidamide is an analogue of Chidamide (CAS 743420-02-0), a hitsone deacetylase inhibitor (HDACI) that enhances gemcitabine (G305000) cytotoxicity in pancreatic cancer cells.

Synthesis

The scalable synthetic approach to chidamide very closely follows the discovery route. The sequence began with the condensation of commercial nicotinaldehyde (52) and malonic acid (53) in a mixture of pyridine and piperidine. Next, activation of acid 54 with N,N0-carbonyldiimidazole (CDI) and subsequent reaction with 4-aminomethyl benzoic acid (55) under basic conditions afforded amide 56 in 82% yield. Finally, activation of 56 with CDI prior to treatment with 4-fluorobenzene- 1,2-diamine (57) and subsequent treatment with TFA and THF yielded chidamide (VIII) in 38% overall yield from 52. However, no publication reported that mono-N-Boc-protected bis-aniline was used to approach Chidamide.

Synthesis_743420-02-2

Chidamide Preparation Products And Raw materials

Raw materials

3,4-Diaminofluorobenzene (E)-4-((3-(pyridin-3-yl)acrylaMido)Methyl)benzoic acid

Preparation Products

Chidamide Suppliers

Global( 130)Suppliers

Supplier	Tel	Country	ProdList	Advantage	Inquiry
CLEARSYNTH LABS LTD.	+91-22-45045900	Hyderabad, India	6351	58	Inquiry
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	China	32836	60	Inquiry
career henan chemical co	+86-0371-86658258 +8613203830695	China	29888	58	Inquiry
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	United States	19892	58	Inquiry
Win-Win chemical CO., Limited	+86-0086-577-64498589 +86-15355981851	China	14351	58	Inquiry
Dideu Industries Group Limited	+86-29-89586680 +86-15129568250	China	24200	58	Inquiry
InvivoChem	+1-708-310-1919 +1-13798911105	United States	6393	58	Inquiry
Coresyn Pharmatech Co., Ltd.	+86-571-86626709 +86-18157142896	China	9991	58	Inquiry
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	China	3136	58	Inquiry
ShenZhen Trendseen Biological Technology Co.,Ltd.	13417589054	China	11681	58	Inquiry

Supplier	Advantage
CLEARSYNTH LABS LTD.	58
ATK CHEMICAL COMPANY LIMITED	60
career henan chemical co	58
TargetMol Chemicals Inc.	58
Win-Win chemical CO., Limited	58
Dideu Industries Group Limited	58
InvivoChem	58
Coresyn Pharmatech Co., Ltd.	58
Nantong HI-FUTURE Biology Co., Ltd.	58
ShenZhen Trendseen Biological Technology Co.,Ltd.	58

Chidamide Spectrum

Chidamide(743420-02-2)MS

743420-02-2(Chidamide)Related Search:

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(E)-N-(2-amino-5-fluorophenyl)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzamide Chidamide Chidamide (E)-N-(2-aMino-5-fluorophenyl)-4-((3-(pyridin-3-yl)acrylaMido)Methyl)benzaMide N-(2-Amino-5-fluorophenyl)-4-[[[1-oxo-3-(3-pyridinyl)-2-propenyl]amino]methyl]benzamide De-4-fluoro 5-Fluoro Chidamide CHIDAMIDE;(E)-N-(2-AMINO-5-FLUOROPHENYL)-4-((3-(PYRIDIN-3-YL)ACRYLAMIDO)METHYL)BENZAMIDE;(E)-N-(2-AMINO-5-FLUOROPHENYL)-4-((3-(PYRIDIN-3-YL)ACRYLAMIDO)METHYL)BENZAMIDE CHIDAMIDE;N-(2-AMINO-5-FLUOROPHENYL)-4-[[[1-OXO-3-(3-PYRIDINYL)-2-PROPENYL]AMINO]METHYL N-(2-Amino-5-fluorophenyl)-4-[[[1-oxo-3-(3-pyridinyl)-2-propenyl]amino]methyl Chidamide D4 Tucidinostat (Chidamide) chidamide analog Chidamide(CS055 CS-1764 HBI-8000) Chidamide,HBI-8000, CS-055, >96% Chidamide impurity HDAC-IN-7 Benzamide, N-(2-amino-5-fluorophenyl)-4-[[[1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]- Chidamide，HBI-8000， CS-055 Chidamide USP/EP/BP N-(2-Amino-5-fluorophenyl)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzamide Benzamide,N-(2-amino-5-fluorophenyl)-[[[1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl] N - (2-amino-5-fluorophenyl) -4- ((3- (pyridin-3-yl) acrylamide) methyl) benzamide 743420-02-2 Inhibitors API