129765-95-3

Usage

Uses

Used in Pharmaceutical Industry:
3-TERT-BUTOXYCARBONYLAMINO-3-METHYL-BUTYRIC ACID is used as an intermediate in the synthesis of (2E)-5-(tert-Butyloxycarbonylamino)-5-methylhex-2-enoic Acid (B809765) for the preparation of C-terminal sulfonamide analogs of NN703. These analogs serve as growth hormone secretagogues, which are compounds that stimulate the release of growth hormone in the body.
The application of 3-TERT-BUTOXYCARBONYLAMINO-3-METHYL-BUTYRIC ACID in the pharmaceutical industry is primarily due to its role in the synthesis of growth hormone secretagogues, which have potential therapeutic applications in the treatment of various conditions related to growth hormone deficiency or imbalance.

Upstream product

• 625-05-8 3-amino-3-methylbutanoic acid 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 874942-30-0 [1,1-dimethyl-2-(1-methyl-1-phenyl-ethylcarbamoyl)-ethyl]-carbamic acid tert-butyl ester 
• 885693-30-1 [3-(4-{4-[(4-cyano-1H-imidazole-2-carbonyl)amino]-3-cyclohex-1-enylphenyl}piperidin-1-yl)-1,1-dimethyl-3-oxopropyl]carbamic acid tert-butyl ester 
• 848644-08-6 {3-[3-(4-chloro-phenoxy)-azetidin-1-yl]-1,1-dimethyl-3-oxo-propyl}-carbamic acid tert-butyl ester 
• 1426680-68-3 methyl N-(tert-butoxycarbonyl)-5,5-dimethyl-3-phenyl-Δ²-pyrroline-2-carboxylate 
• 1426444-02-1 tert-butyl 2-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)propan-2-ylcarbamate 
• 193079-05-9 (E)-5-Amino-5-methyl-hex-2-enoic acid ((R)-1-{[(R)-1-((R)-2-hydroxy-propylcarbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-naphthalen-2-yl-ethyl)-methyl-amide 
• 193079-05-9 (E)-5-Amino-5-methyl-hex-2-enoic acid ((R)-1-{[(R)-1-((S)-2-hydroxy-propylcarbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-naphthalen-2-yl-ethyl)-methyl-amide 
• 213335-92-3 {(E)-4-[((R)-1-{[(R)-1-((R)-2-Hydroxy-propylcarbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-naphthalen-2-yl-ethyl)-methyl-carbamoyl]-1,1-dimethyl-but-3-enyl}-carbamic acid tert-butyl ester 
• 213335-84-3 {(E)-4-[((R)-1-{[(R)-1-((S)-2-Hydroxy-propylcarbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-naphthalen-2-yl-ethyl)-methyl-carbamoyl]-1,1-dimethyl-but-3-enyl}-carbamic acid tert-butyl ester 
• 1027896-29-2 {(E)-4-[((R)-2-Biphenyl-4-yl-1-{[(R)-2-(4-fluoro-phenyl)-1-((R)-2-hydroxy-propylcarbamoyl)-ethyl]-methyl-carbamoyl}-ethyl)-methyl-carbamoyl]-1,1-dimethyl-but-3-enyl}-carbamic acid tert-butyl ester 
• 193085-86-8 ((E)-1,1-Dimethyl-4-{methyl-[(R)-1-(methyl-{(R)-2-phenyl-1-[(tetrahydro-furan-2-ylmethyl)-carbamoyl]-ethyl}-carbamoyl)-2-naphthalen-1-yl-ethyl]-carbamoyl}-but-3-enyl)-carbamic acid tert-butyl ester 
• 213335-86-5 ((E)-1,1-Dimethyl-4-{methyl-[(R)-1-(methyl-{(R)-2-phenyl-1-[(tetrahydro-furan-2-ylmethyl)-carbamoyl]-ethyl}-carbamoyl)-2-naphthalen-2-yl-ethyl]-carbamoyl}-but-3-enyl)-carbamic acid tert-butyl ester 
• 1026241-86-0 {(E)-4-[((R)-2-Biphenyl-4-yl-1-{[(R)-1-((S)-2-hydroxy-propylcarbamoyl)-2-thiophen-2-yl-ethyl]-methyl-carbamoyl}-ethyl)-methyl-carbamoyl]-1,1-dimethyl-but-3-enyl}-carbamic acid tert-butyl ester 
• 213335-88-7 {(E)-4-[((R)-1-{[(R)-1-(Cyclopropylmethyl-carbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-naphthalen-2-yl-ethyl)-methyl-carbamoyl]-1,1-dimethyl-but-3-enyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

NOVEL FERROPORTIN INHIBITORS

The invention relates to novel ferroportin inhibitors of the general formula (I) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β- hydroxysteroid dehydrogenase 1 inhibitor

Many adamantane derivatives have been demonstrated to function as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. 3-Amino-N-adamantyl-3-methylbutanamide derivatives were optimized by structure-based drug design. Compound 8j exhibited a good in vitro and ex vivo inhibitory activity against both human and mouse 11β-HSD1.

Synthesis of racemic δ,δ-dimethylproline derivatives

A versatile methodology for the preparation of racemic δ,δ- dimethylproline derivatives has been developed. Methyl N-Boc-δ,δ- dimethylprolinate was synthesized from a β-amino acid in six steps and 55 % overall yield. The route is amenable to the preparation of a broad range of δ,δ-disubstituted prolines by starting with the adequate β-amino acids. In addition, one of the intermediate compounds in the synthetic route has been used for the preparation of a δ,δ- dimethylproline derivative that is substituted at the β-position with a phenyl group. This has been achieved by coupling phenylboronic acid with a regioselectively generated vinyl triflate followed by a stereoselective hydrogenation. δ,δ-Dimethylproline derivatives have been efficiently synthesized by employing a β-amino acid as the starting material. The methodology is amenable to the preparation of other δ,δ- disubstituted prolines. Copyright

NOVEL PYRIDINE DERIVATIVES

The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

PYRIDIN- 2 -AMIDES USEFUL AS CB2 AGONISTS

The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

PIPERIDINYL DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present application describes modulators of MIP-1α of formula (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators of formula (I) are disclosed.