180253-66-1

Usage

Uses

Used in Pharmaceutical Research:
3-(BOC-AMINO)-4-PICOLINE is used as a key intermediate in the synthesis of various pharmaceuticals. Its presence of the BOC protecting group allows for the controlled formation of peptide bonds, facilitating the development of new drug candidates with potential therapeutic applications.
Used in Agrochemical Production:
In the agrochemical industry, 3-(BOC-AMINO)-4-PICOLINE is utilized as a building block for the synthesis of bioactive compounds. Its unique structure and reactivity contribute to the creation of novel agrochemicals with improved efficacy and selectivity in pest control and crop protection.
Used in Organic Synthesis:
3-(BOC-AMINO)-4-PICOLINE is employed as a reagent in the preparation of various organic compounds. Its versatility in organic synthesis allows for the development of new chemical entities with potential applications in materials science, chemical biology, and other related fields.
Overall, 3-(BOC-AMINO)-4-PICOLINE is an important chemical with diverse applications in the field of organic synthesis and pharmaceutical research, contributing to the advancement of new drug development, agrochemical innovation, and the synthesis of novel organic compounds.

InChI:InChI=1/C12H18N2O2/c1-12(2,3)16-11(15)14-10-7-5-4-6-9(10)8-13/h4-7H,8,13H2,1-3H3,(H,14,15)/p+1

Upstream product

• 56700-70-0 3-(tert-butoxycarbonylamino)pyridine 
• 74-88-4 methyl iodide 
• 3430-27-1 3-amino-4-methylpyridine 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1070-89-9 sodium hexamethyldisilazane 
• 4248-19-5 tert-butyl carbazate 
• 3430-22-6 3-Bromo-4-methylpyridin 
• 1990-90-5 4-amino-3-methylpyridine 

Downstream Products

• 264883-51-4 2-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-6-azaindole 
• 264883-52-5 methyl 2-Methoxy-4-[[2-[4-[2-(1-pyrrolidinyl)ethoxy]-phenyl]-6-azaindol-1-yl]methyl]benzoate 
• 945608-00-4 2-phenylpyrrolo[2,3-c]pyridine-1-carboxylic acid tert-butyl ester 
• 24334-19-8 ethyl 1H-pyrrolo[2,3-c]pyridine-2-carboxylate 
• 454709-84-3 tert-butyl (trans)-4-methyl-3-piperidinylcarbamate 
• 1374239-65-2 1-(3-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-4-methylpiperidin-1-yl)-2-(3,5-dichlorophenylamino)ethanone 
• 1374243-23-8 tert-butyl 1-(2-(3,5-dichlorophenylamino)acetyl)-4-methylpiperidin-3-ylcarbamate 
• 1374243-24-9 1-(3-amino-4-methylpiperidin-1-yl)-2-(3,5-dichlorophenylamino)ethanone 
• 1374243-25-0 2-(3,5-dichlorophenylamino)-1-(4-methyl-3-(7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)ethanone 
• 250275-20-8 cis-tert-butyl (4-methylpiperidin-3-yl)carbamate 
• 101084-17-7 4-ethyl-[3]pyridylamine 

Relevant academic research and scientific papers

HETEROCYCLIC COMPOUNDS

The invention provides new heterocyclic compounds having the general formula (I) wherein A, L, Q, U, V, W, X, Z, m, n, and R1 to R4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

COMPOUNDS FOR USING IN IMAGING AND PARTICULARLY FOR THE DIAGNOSIS OF NEURODEGENERATIVE DISEASES

The invention relates to compounds of formula (II) for using in imaging and particularly for the diagnosis of neurodegenerative diseases

The Excited-State Triple Proton Transfer Reaction of 2,6-Diazaindoles and 2,6-Diazatryptophan in Aqueous Solution

3-Me-2,6-diazaindole ((2,6-aza)Ind) was strategically designed and synthesized to probe water molecule catalyzed excited-state proton transfer in aqueous solution. Upon electronic excitation (λmax ～ 300 nm), (2,6-aza)Ind undergoes N(1)-H to N(6) long-distance proton transfer in neutral H2O, resulting in normal (340 nm) and proton-transfer tautomer (480 nm) emissions with an overall quantum yield of 0.25. The rate of the water-catalyzed proton transfer shows a prominent H/D kinetic isotope effect, which is determined to be 8.3 × 108 s-1 and 4.7 × 108 s-1 in H2O and D2O, respectively. Proton inventory experiments indicate the involvement of two water molecules and three protons, which undergo a relay type of excited-state triple proton transfer (ESTPT) in a concerted, asynchronous manner. The results demonstrate for the first time the fundamental of triple proton transfer in pure water for azaindoles as well as pave a new avenue for 2,6-diazatryptophan, an analogue of tryptophan exhibiting a similar ESTPT property with (2,6-aza)Ind, to probe biowaters in proteins.

Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors

High levels of Pim expression have been implicated in several hematopoietic and solid tumor cancers, suggesting that inhibition of Pim signaling could provide patients with therapeutic benefit. Herein, we describe our progress towards this goal using a screening hit (rac-1) as a starting point. Modification of the indazole ring resulted in the discovery of a series of imidazopyridazine-based Pim inhibitors exemplified by compound 22m, which was found to be a subnanomolar inhibitor of the Pim-1 and Pim-2 isoforms (IC50values of 0.024?nM and 0.095?nM, respectively) and to potently inhibit the phosphorylation of BAD in a cell line that expresses high levels of all Pim isoforms, KMS-12-BM (IC50?=?28?nM). Profiling of Pim-1 and Pim-2 expression levels in a panel of multiple myeloma cell lines and correlation of these data with the potency of compound 22m in a proliferation assay suggests that Pim-2 inhibition would be advantageous for this indication.

ANNELATED PYRROLES AND THEIR USE AS CRAC INHIBITORS

The invention relates to substituted bicyclic pyrroloheterocyclyl compounds of general formula (I), wherein A1 and A2 represent direct bond or C(=O), with the proviso that 0 or 1 of A1 and A2 represents C(=O); m and n independently denote 0, 1, 2 or 3, with the proviso that the sum [n + m] is 1, 2, 3 or 4; R1 denotes H, F, CI, Br, I, CN, CF3, CF2H, CFH2, CO2H, CO2R13, R13, OH. O-R13, NH2, N(H)R13, N(R13)2, R2 represents 0 to 4 substituents, each independently selected from F, CI, Br, CN. CF3, CF2H, CFH2, R13, OH, O-R13, NH2, N(H)R13 and N(R13)2; Ar1 represents phenyl or 5- or 6-membered heteroaryl, in each case unsubstituted or substituted with one, two, three or four substituents, independently selected from F, CI, Br, CN, CF3. CF2H, CFH2, R13 and O- R13; or C3-6-cycloalkyl or 3 to 7 membered heterocycloalkyl, in each case unsubstituted or mono- or polysubstituted; Ar2 represents phenyl or 5- or 6-membered heteroaryl, wherein said phenyl or said heteroaryl may be unsubstituted or mono- or polysubstituted and may be condensed with a 4-, 5-, 6-or 7- membered ring, being carbocyclic or heterocyclic, wherein said condensed ring may be saturated, partially unsaturated or aromatic and may be unsubstituted or mono- or polysubstituted; useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.

BICYCLIC PYRIDAZINE COMPOUNDS AS PIM INHIBITORS

The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

HETEROCYCLIC TYROSINE KINASE INHIBITORS

The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same. In certain embodiments, the present invention provides pharmaceutical formulations comprising provided compounds. In certain embodiments, the present invention provides a method of decreasing enzymatic activity of a Tec kinase family member. In some embodiments, such methods include contacting a Tec kinase family member with an effective amount of a Tec kinase family member inhibitor. In certain embodiments, the present invention provides a method of treating a disorder responsive to Tec kinase family inhibition in a subject in need thereof.

IMIDAZOPYRIDINE DERIVATIVES AS JAK INHIBITORS

New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

Imidazopyridine derivatives as JAK inhibitors

New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

Pd-catalyzed amidation of aryl(Het) halides with tert-butyl carbamate

Pd-catalyzed cross-coupling reaction of tert-butyl carbamate with various aryl(Het) halides with Cs2CO3 as base in 1,4-dioxane as solvent was investigated, which resulted in the formation of the desired compounds in moderate to excellent yields.