115378-33-1

Upstream product

• 913344-40-8 tert-butyl N-formyl carbamate 
• 129076-07-9 (-)-di-tert-butyl [(1S)-1-methylprop-2-en-1-yl]imidodicarbonate 
• 1033286-96-2 (S)-tert-butyl formyl(1-methylprop-2-en-1-yl)carbamate 
• 79069-50-4 Boc-Ala-H 
• 28875-17-4 (S)-N-(tert-butoxycarbonyl)alanine methyl ester 
• 154079-54-6 (2S,3S)-3-tert-butoxycarbonylamino-1,2-butanediol 
• 1779-49-3 Methyltriphenylphosphonium bromide 
• 75-11-6 diiodomethane 

Downstream Products

• 1609651-47-9 C₂₂H₂₄FN₃O₂ 
• 106539-14-4 (S)-methyl 3-(tert-butyloxycarbonylamino)butyrate 
• 357385-69-4 1(R,S)-[1'(S)-tert-butyloxycarbonylaminoethyl]oxirane 
• 106539-36-0 tert-butyl N-[(2S)-4-hydroxybutan-2-yl]carbamate 
• 79069-13-9 (S)-2-t-butoxycarbonylaminopropan-1-ol 

Relevant academic research and scientific papers

Discovery of DS79932728: A Potent, Orally Available G9a/GLP Inhibitor for Treating β-Thalassemia and Sickle Cell Disease

Therapeutic reactivation of the γ-globin genes for fetal hemoglobin (HbF) production is an attractive strategy for treating β-thalassemia and sickle cell disease. It was reported that genetic knockdown of the histone lysine methyltransferase EHMT2/1 (G9a/GLP) is sufficient to induce HbF production. The aim of the present work was to acquire a G9a/GLP inhibitor that induces HbF production sufficiently. It was revealed that tetrahydroazepine has versatility as a side chain in various skeletons. We ultimately obtained a promising aminoindole derivative (DS79932728), a potent and orally bioavailable G9a/GLP inhibitor that was found to induce γ-globin production in a phlebotomized cynomolgus monkey model. This work could facilitate the development of effective new approaches for treating β-thalassemia and sickle cell disease.

MACROCYCLIC SPIROETHERS AS MCL-1 INHIBITORS

Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

AMINO SULFONYL COMPOUNDS

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING AMINO SULFONYL LINKAGE

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Iridium-catalyzed asymmetric allylic substitutions with bulky amines/oxidative double bond cleavage - Entry into the reetz synthesis of amino alcohols

Branched allylic amines were prepared by Ir-catalyzed enantioselective allylic aminations with the bulky N-nucleophiles HN(Boc)2 and HNBn2. The products were transformed into N-protected amino aldehydes, which were either reduced or coupled diastereoselectively with organometallic compounds to give vicinal amino alcohols. A formal synthesis of the neurokinin receptor antagonist (+)-L-733060 was carried out as an application. Ir-catalyzed enantioselective allylic aminations with bulky N-nucleophiles HN(Boc)2 and HNBn2 gave N-protected allylic amines, which were transformed into N-protected chiral amino aldehydes. These are useful chiral building blocks as previously demonstrated by Reetz et al. A formal synthesis of the neurokinin receptor antagonist (+)-L-733060 was carried out as an application.

Synthesis of chiral, enantiopure allylic amines by the Julia olefination of α-amino esters

The four-step conversion of a series of N-Boc-protected L-amino acid methyl esters into enantiopure N-Boc allylamines by a modified Julia olefination is described. Key steps include the reaction of a lithiated phenylalkylsulfone with amino esters, giving chiral β-ketosulfones, and the reductive elimination of related α-acetoxysulfones. The overall transformation takes place under mild conditions, with good yields, and without loss of stereochemical integrity, being in this respect superior to the conventional Julia reaction of α-amino aldehydes.

The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation

We report the discovery of highly potent and selective non-steroidal glucocorticoid receptor modulators with PK properties suitable for inhalation. A high throughput screen of the AstraZeneca compound collection identified sulfonamide 3 as a potent non-steroidal glucocorticoid receptor ligand. Further optimization of this lead generated indazoles 30 and 48 that were progressed to characterization in in vivo models. X-ray crystallography was used to gain further insight into the binding mode of selected ligands.

Stereoselective synthesis of a lactam analogue of brefeldin C

A convergent, stereoselective synthesis of a brefeldin C lactam analogue is described. Novel features are application of the asymmetric iridium-catalyzed allylic substitution on a multigram scale for construction of the stereogenic centers C-9 as well as C-15 and an intermolecular Nozaki-Hiyama-Kishi reaction for introduction of the brefeldin enoate moiety. Georg Thieme Verlag Stuttgart.

INDAZOLYL SULPHONAMIDE DERIVATIVES FOR THE TREATMENT OF GLUCOCORTICOID RECEPTOR MEDIATED DISORDERS

Compounds of formula (I): [Chemical formula should be inserted here. Please see paper copy] or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal)

NOVEL BICYCLIC SULFONAMIDES FOR USE AS GLUCOCORTICOID RECEPTOR MODULATORS IN THE TREATMENT OF INFLAMMATORY DISEASES

Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).