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870-46-2 Usage

Chemical Properties

White to pale yellow lumps

Uses

Different sources of media describe the Uses of 870-46-2 differently. You can refer to the following data:
1. Starting material for preparing BOC-azide, a reagent to introduce the BOC amino protection.
2. tert-Butyl carbazate is used in a palladium-catalyzed cross-coupling with vinyl halides to prepare N-Boc-N-alkenylhydrazines. It is utilized in solid phase peptide synthesis and in the optical purity determination of alfa-amino aldehyde. It reacts with aldehydes to get hydrazones, which finds application as an intermediate in the synthesis of HIV-1 protease inhibitors. In addition to this, it is used as a starting material for the preparation of BOC-azide, sulfonic and carboxylic hydrazides.

Synthesis Reference(s)

Journal of the American Chemical Society, 82, p. 2725, 1960 DOI: 10.1021/ja01496a018Chemical and Pharmaceutical Bulletin, 18, p. 217, 1970 DOI: 10.1248/cpb.18.217

Purification Methods

Distil it in a Claisen flask with a water or oil bath at ca 80o. After a couple of drops have distilled, the carbazate is collected as an oil which solidifies to a snow white solid. It can be crystallised with 90% recovery from a 1:1 mixture of pet ether (b 30-60o) and pet ether (b 60-70o). [Carpino et al. Org Synth Coll Vol V 166 1973, Caprino et al. Org Synth 44 20 1964, Beilstein 3 IV 175.]

Check Digit Verification of cas no

The CAS Registry Mumber 870-46-2 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 8,7 and 0 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 870-46:
(5*8)+(4*7)+(3*0)+(2*4)+(1*6)=82
82 % 10 = 2
So 870-46-2 is a valid CAS Registry Number.
InChI:InChI=1/C5H12N2O2/c1-5(2,3)7(6)4(8)9/h6H2,1-3H3,(H,8,9)/p-1

870-46-2 Well-known Company Product Price

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  • TCI America

  • (C0933)  tert-Butyl Carbazate  >97.0%(T)

  • 870-46-2

  • 25g

  • 286.00CNY

  • Detail
  • TCI America

  • (C0933)  tert-Butyl Carbazate  >97.0%(T)

  • 870-46-2

  • 250g

  • 1,520.00CNY

  • Detail
  • Alfa Aesar

  • (A12383)  tert-Butyl carbazate, 98+%   

  • 870-46-2

  • 25g

  • 376.0CNY

  • Detail
  • Alfa Aesar

  • (A12383)  tert-Butyl carbazate, 98+%   

  • 870-46-2

  • 100g

  • 858.0CNY

  • Detail
  • Alfa Aesar

  • (A12383)  tert-Butyl carbazate, 98+%   

  • 870-46-2

  • 500g

  • 3624.0CNY

  • Detail
  • Aldrich

  • (B91005)  tert-Butylcarbazate  98%

  • 870-46-2

  • B91005-5G

  • 296.01CNY

  • Detail
  • Aldrich

  • (B91005)  tert-Butylcarbazate  98%

  • 870-46-2

  • B91005-25G

  • 470.34CNY

  • Detail
  • Aldrich

  • (B91005)  tert-Butylcarbazate  98%

  • 870-46-2

  • B91005-100G

  • 2,434.77CNY

  • Detail
  • Aldrich

  • (B91005)  tert-Butylcarbazate  98%

  • 870-46-2

  • B91005-500G

  • 3,856.09CNY

  • Detail

870-46-2SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name tert-Butyl carbazate

1.2 Other means of identification

Product number -
Other names tert-butyl N-aminocarbamate

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:870-46-2 SDS

870-46-2Synthetic route

tert-butyl phenyl carbonate
6627-89-0

tert-butyl phenyl carbonate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate Heating;100%
With hydrazine hydrate
tert-butyl 2,2,2-trichloroethyl hydrazine-1,2-dicarboxylate

tert-butyl 2,2,2-trichloroethyl hydrazine-1,2-dicarboxylate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With chloro-trimethyl-silane; mischmetal (50 percent Ce, 25 percent La, 16 percent Nd, 6 percentPr) In tetrahydrofuran for 2h; Heating;99%
di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate97%
With hydrazine hydrate In isopropyl alcohol at 0℃; for 2h;97%
With potassium carbonate; hydrazine hydrate In 1,4-dioxane; water at 20℃; for 12h;93%
S-Methyl-monothiokohlensaeure-tert.-butylester
29518-83-0

S-Methyl-monothiokohlensaeure-tert.-butylester

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With water; hydrazine
With hydrazine
tert-butyl 2,2,2-trichloroacetate
1860-21-5

tert-butyl 2,2,2-trichloroacetate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate In N,N-dimethyl-formamide
α-Nitroisobuttersaeure-tert-butylester
99969-78-5

α-Nitroisobuttersaeure-tert-butylester

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine
tert-butyl cyanoformate
57022-34-1

tert-butyl cyanoformate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate at 5℃;
benzyl tert-butyl carbonate
60470-15-7

benzyl tert-butyl carbonate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate In isopropyl alcohol
tert-Butyl-N-nitrocarbamat
68058-85-5

tert-Butyl-N-nitrocarbamat

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
With hydrazine hydrate
phosgene
75-44-5

phosgene

tert-butyl alcohol
75-65-0

tert-butyl alcohol

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
(i) Py, Et2O, (ii) N2H4*H2O, Et2O; Multistep reaction;
N,1'-bis[(1,1-dimethylethoxy)carbonyl]-L-histidine
20866-46-0

N,1'-bis[(1,1-dimethylethoxy)carbonyl]-L-histidine

A

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

B

N-(tert-butoxycarbonyl)-L-histidine
17791-52-5

N-(tert-butoxycarbonyl)-L-histidine

Conditions
ConditionsYield
In ethanol for 0.166667h; Heating; Yield given. Yields of byproduct given;
tert-butyl carbamate
4248-19-5

tert-butyl carbamate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: (i) Cu(NO3)2*3H2O, Ac2O, Hg(OAc)2, (ii) H2S, acetone
2: N2H4*H2O
View Scheme
sodium t-butyl carbonate

sodium t-butyl carbonate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: KI / petroleum ether; dimethylformamide
2: N2H4*H2O / propan-2-ol
View Scheme
tert-butyl acetoacetate
1694-31-1

tert-butyl acetoacetate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
Stage #1: tert-butyl acetoacetate With potassium tert-butylate In tetrahydrofuran at 0℃; for 1h; Inert atmosphere;
Stage #2: With 1-bromo-4-butene; sodium iodide In tetrahydrofuran at 0℃; for 12h; Inert atmosphere; Reflux;
di-tert-butyl dicarbonate
24424-99-5

di-tert-butyl dicarbonate

hydrazine
302-01-2

hydrazine

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
In dichloromethane
tert-butyl hydrogen carbonate
51300-90-4

tert-butyl hydrogen carbonate

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

Conditions
ConditionsYield
Stage #1: tert-butyl hydrogen carbonate With sulfuric acid In methanol at 20℃; for 4h; Reflux;
Stage #2: With hydrazine hydrate In methanol at 75℃; for 0.5h;
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N-(tert-butyloxycarbonyl) azide
1070-19-5

N-(tert-butyloxycarbonyl) azide

Conditions
ConditionsYield
With acetic acid; sodium nitrite In water at 0 - 20℃; for 2.08333h;100%
With potassium hydrogencarbonate; sodium nitrite In water; acetic acid97%
With acetic acid; sodium nitrite at 0℃; for 30h;92%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

benzaldehyde
100-52-7

benzaldehyde

t-butyl 3-benzylidenecarbazate
24469-50-9

t-butyl 3-benzylidenecarbazate

Conditions
ConditionsYield
In tetrahydrofuran at 20℃; for 4h;100%
In ethanol for 3h; Reflux;100%
In ethanol99%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

acetone
67-64-1

acetone

tert-butyl isopropylidenecarbazate
16689-34-2

tert-butyl isopropylidenecarbazate

Conditions
ConditionsYield
for 4h; Heating;100%
at 50℃;100%
at 60℃; Temperature;100%
5-nitrofurane-2-carboxaldehyde
698-63-5

5-nitrofurane-2-carboxaldehyde

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N'-tert-butyl-2-((5-nitrofuran-2-yl)methylene)hydrazinecarboxylate

N'-tert-butyl-2-((5-nitrofuran-2-yl)methylene)hydrazinecarboxylate

Conditions
ConditionsYield
for 0.25h; Heating;100%
In ethanol at 20℃;65%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

cyclopentanone
120-92-3

cyclopentanone

tert-butyl 2-cyclopentylidenehydrazine carboxylate
79201-39-1

tert-butyl 2-cyclopentylidenehydrazine carboxylate

Conditions
ConditionsYield
In methanol at 20℃; for 2h;100%
In methanol at 20℃; for 3h; Inert atmosphere;98%
In hexane for 0.333333h; Heating;96%
thiophene-2-carbaldehyde
98-03-3

thiophene-2-carbaldehyde

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

(E)-tert-butyl 2-(thiophen-2-ylmethylene)hydrazinecarboxylate
180462-80-0

(E)-tert-butyl 2-(thiophen-2-ylmethylene)hydrazinecarboxylate

Conditions
ConditionsYield
at 20℃; for 1.5h; Neat (no solvent); Ball-milling;100%
In ethanol for 3h; Heating;97%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

isobutyraldehyde
78-84-2

isobutyraldehyde

N'-(2-methylpropylidene)hydrazinecarboxylic acid tert-butyl ester
57699-46-4

N'-(2-methylpropylidene)hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In toluene at 50℃; for 1h;100%
In methanol at 20℃; for 1h;100%
In methanol at 20℃; for 1h; Inert atmosphere;100%
In ethanol for 3h; Heating;99%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

isovaleraldehyde
590-86-3

isovaleraldehyde

N'-(3-methylbutylidene)hydrazinecarboxylic acid tert-butyl ester

N'-(3-methylbutylidene)hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In toluene at 50℃; for 1h;100%
In ethanol for 3h; Heating;81%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

cyclohexanecarbaldehyde
2043-61-0

cyclohexanecarbaldehyde

(E)-tert-butyl 2-(cyclohexylmethylene)hydrazinecarboxylate
929016-50-2

(E)-tert-butyl 2-(cyclohexylmethylene)hydrazinecarboxylate

Conditions
ConditionsYield
In ethanol for 3h; Heating;100%
In methanol at 20℃; for 1h; Inert atmosphere;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

(S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid
162537-11-3

(S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid

(S)-N'-(2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazinecarboxylic acid tert-butyl ester
198904-77-7

(S)-N'-(2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
With 4-methyl-morpholine; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In ethyl acetate; N,N-dimethyl-formamide at 20℃; for 18.75h;100%
Stage #1: (S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride at 20℃; for 0.166667h; Inert atmosphere;
Stage #2: With 4-methyl-morpholine; benzotriazol-1-ol for 0.5h; Inert atmosphere;
Stage #3: t-butoxycarbonylhydrazine at 20℃; for 20h; Inert atmosphere;
94%
Stage #1: (S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoic acid With benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In DMF (N,N-dimethyl-formamide) at 25℃; for 0.25h;
Stage #2: t-butoxycarbonylhydrazine With 4-methyl-morpholine In DMF (N,N-dimethyl-formamide) at 25℃; for 16h;
90%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

4-Phenylbenzaldehyde
3218-36-8

4-Phenylbenzaldehyde

N'-[1-Biphenyl-4-yl-meth-(E)-ylidene]-hydrazinecarboxylic acid tert-butyl ester

N'-[1-Biphenyl-4-yl-meth-(E)-ylidene]-hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In ethanol for 4h; Heating;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

methyl (2E)-6-oxoundeca-2,10-dienoate
319491-31-1

methyl (2E)-6-oxoundeca-2,10-dienoate

6-(tert-butoxycarbonyl-hydrazono)-undeca-2,10-dienoic acid methyl ester

6-(tert-butoxycarbonyl-hydrazono)-undeca-2,10-dienoic acid methyl ester

Conditions
ConditionsYield
In diethyl ether at 5℃; for 12h;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

2-Naphthalenesulfonyl chloride
93-11-8

2-Naphthalenesulfonyl chloride

C15H18N2O4S

C15H18N2O4S

Conditions
ConditionsYield
Substitution;100%
phthalic anhydride
85-44-9

phthalic anhydride

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

1-tert-butyloxycarbonyl-2-(2'-carboxybenzoyl)-hydrazine
215655-64-4

1-tert-butyloxycarbonyl-2-(2'-carboxybenzoyl)-hydrazine

Conditions
ConditionsYield
In tetrahydrofuran at 20℃; for 0.0833333h; Acylation; ring cleavage;100%
furfural
98-01-1

furfural

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N'-(furan-2-ylmethylene)hydrazinecarboxylic acid tert-butyl ester
113906-60-8

N'-(furan-2-ylmethylene)hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
at 20℃; for 1h; Neat (no solvent); Ball-milling;100%
In tetrahydrofuran96%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

benzaldehyde
100-52-7

benzaldehyde

N'-(phenylmethylene)hydrazinecarboxylic acid tert-butyl ester
24469-50-9

N'-(phenylmethylene)hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
at 20℃; for 0.75h; Neat (no solvent); Ball-milling;100%
In toluene at 20℃;93%
In tetrahydrofuran at 20℃; for 4h;88%
Tetrahydro-4H-pyran-4-one
29943-42-8

Tetrahydro-4H-pyran-4-one

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N’-(tetrahydropyran-4-ylidene)hydrazinecarboxylic acid tert-butyl ester
693287-78-4

N’-(tetrahydropyran-4-ylidene)hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In methanol at 20℃;100%
In methanol at 20℃;100%
In hexanes at 65 - 70℃; for 1.5h;79%
Tetrahydrothiopyran-4-one
1072-72-6

Tetrahydrothiopyran-4-one

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

tert-butyl 2-(tetrahydro-4H-thiopyran-4-ylidene)hydrazinecarboxylate
693287-85-3

tert-butyl 2-(tetrahydro-4H-thiopyran-4-ylidene)hydrazinecarboxylate

Conditions
ConditionsYield
In methanol at 20℃;100%
In methanol at 20℃; for 4h;
In methanol
cycloactanone
502-49-8

cycloactanone

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N'-cyclooctylidene-hydrazinecarboxylic acid tert-butyl ester
339058-79-6

N'-cyclooctylidene-hydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In methanol at 20℃;100%
diisobutyl ketone
108-83-8

diisobutyl ketone

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N-[1-aza-4-methyl-2-(2-methylpropyl)pent-1-enyl](tert-butoxy)carboxamide
693288-00-5

N-[1-aza-4-methyl-2-(2-methylpropyl)pent-1-enyl](tert-butoxy)carboxamide

Conditions
ConditionsYield
In methanol at 20℃;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

2,6-difluoro-thiobenzimidic acid methyl ester; hydriodide

2,6-difluoro-thiobenzimidic acid methyl ester; hydriodide

N'-[(2,6-difluoro-phenyl)-imino-methyl]-hydrazinecarboxylic acid tert-butyl ester; hydriodide

N'-[(2,6-difluoro-phenyl)-imino-methyl]-hydrazinecarboxylic acid tert-butyl ester; hydriodide

Conditions
ConditionsYield
100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N-ethoxycarbonyl-4-piperidone
29976-53-2

N-ethoxycarbonyl-4-piperidone

4-(tert-butoxycarbonyl-hydrazono)-piperidine-1-carboxylic acid ethyl ester
693287-92-2

4-(tert-butoxycarbonyl-hydrazono)-piperidine-1-carboxylic acid ethyl ester

Conditions
ConditionsYield
In methanol at 20℃;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

cyclohexanecarbaldehyde
2043-61-0

cyclohexanecarbaldehyde

N-((1Z)-1-aza-2-cyclohexylvinyl)(tert-butoxy)carboxamide
654058-77-2

N-((1Z)-1-aza-2-cyclohexylvinyl)(tert-butoxy)carboxamide

Conditions
ConditionsYield
In methanol at 20℃;100%
pentanal
110-62-3

pentanal

t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

N'-pentylidenehydrazinecarboxylic acid tert-butyl ester

N'-pentylidenehydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In toluene at 50℃; for 1h;100%
t-butoxycarbonylhydrazine
870-46-2

t-butoxycarbonylhydrazine

acetaldehyde
75-07-0

acetaldehyde

N'-ethylidenehydrazinecarboxylic acid tert-butyl ester

N'-ethylidenehydrazinecarboxylic acid tert-butyl ester

Conditions
ConditionsYield
In toluene at 50℃; for 1h;100%
In toluene at 20 - 50℃; for 25h;97.5%
In toluene at 20 - 50℃; for 25h;97.5%
In tetrahydrofuran at 18 - 25℃; for 24h;80%

870-46-2Relevant articles and documents

Ovchivnikow et al.

, p. 418 (1965)

Preparation method of high-purity tert-butyl carbazole

-

Paragraph 0029-0036, (2021/09/21)

The invention relates to the technical field of drug synthesis, in particular to a preparation method of high-purity tert-butyl carbazole. After the completion of the reaction, the hydrazine monohydrate is neutralized with a base, extracted with a solvent, concentrated, and then crystallized by a weak polar solvent to give a tert-butyl carbazole product. The preparation method of the tert-butyl carbazole can obtain the high-purity product (≥ 99.5%), has high yield (≥ 90%), is simple to operate, and is suitable for industrial large-scale production.

Elastic targeting polypeptide-based medicine-carrying nanoparticle as well as preparation method and application thereof

-

Paragraph 0029-0031; 0039-0041, (2020/07/15)

The invention discloses an elastic targeting polypeptide-based medicine-carrying nanoparticle. The nanoparticle is prepared from an elastic targeting polypeptide and a modified medicine, wherein the modified medicine is a modified paclitaxel PTX-LEV-MECH or modified salinomycin Sail-ABA-MPBH. The elastic targeting polypeptide-based medicine-carrying nanoparticle provided by the invention is 100nmor below in particle size, so that the dispersion degree is low, the medicine carrying rate is high, and the nanoparticle can be combined with in-vivo albumin for transferring and carrying medicine, and also can be combined with acidic rich cysteine specifically secreted by tumor cells, the drug is concentrated in the acidic environment, the breast cancer in-situ cancer is targeted for killing, and the toxic and side effects of the drug on the whole body are reduced; and the efficacy of treating breast cancer is increased and improved by utilizing the synergistic effect of two nanoparticles, the occurrence of the metastasis of the breast cancer cells through a lymphatic system and a blood system is reduced, and the occurrence of serious complications such as medical-source lymphatic edemacaused by a lymph node sweeping surgery is reduced.

Multiprotein Dynamic Combinatorial Chemistry: A Strategy for the Simultaneous Discovery of Subfamily-Selective Inhibitors for Nucleic Acid Demethylases FTO and ALKBH3

Das, Mohua,Yang, Tianming,Dong, Jinghua,Prasetya, Fransisca,Xie, Yiming,Wong, Kendra H. Q.,Cheong, Adeline,Woon, Esther C. Y.

supporting information, p. 2854 - 2867 (2018/09/25)

Dynamic combinatorial chemistry (DCC) is a powerful supramolecular approach for discovering ligands for biomolecules. To date, most, if not all, biologically templated DCC systems employ only a single biomolecule to direct the self-assembly process. To expand the scope of DCC, herein, a novel multiprotein DCC strategy has been developed that combines the discriminatory power of a zwitterionic “thermal tag” with the sensitivity of differential scanning fluorimetry. This strategy is highly sensitive and could differentiate the binding of ligands to structurally similar subfamily members. Through this strategy, it was possible to simultaneously identify subfamily-selective probes against two clinically important epigenetic enzymes: FTO (7; IC50=2.6 μm) and ALKBH3 (8; IC50=3.7 μm). To date, this is the first report of a subfamily-selective ALKBH3 inhibitor. The developed strategy could, in principle, be adapted to a broad range of proteins; thus it is of broad scientific interest.

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