133625-87-3

Usage

Uses

Acivicin intermediate.

Upstream product

• 75-11-6 diiodomethane 
• 95715-87-0 (R)-3-tert-butoxycarbonyl-4-formyl-2,2-dimethyloxazolidine 
• 19493-09-5 Methylenetriphenylphosphorane 
• 1779-49-3 Methyltriphenylphosphonium bromide 
• 91103-37-6 tert-butyl [(1S)-1-(hydroxymethyl)prop-2-en-1-yl]carbamate 
• 77-76-9 2,2-dimethoxy-propane 
• 95715-87-0 tert-butyl 4-formyl-2,2-dimethyloxazolidine-3-carboxylate 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 24424-99-5 di-tert-butyl dicarbonate 
• 169324-82-7 N-tert-butoxycarbonyl-N-(1-hydroxymethyl-2-propenyl)amine 
• 51372-93-1 (S)-tert-butyl (1-hydroxy-4-(methylthio)butan-2-yl)carbamate 
• 108149-60-6 methyl [(4R)-3-(tert-butoxycarbonyl)-2,2-dimethyl-1,3-oxazolidin-4-yl]carboxylate 
• 109-72-8 n-butyllithium 
• 2766-43-0 N-tert-butyloxycarbonyl-L-serine methyl ester 

Downstream Products

• 91103-37-6 tert-butyl [(1S)-1-(hydroxymethyl)prop-2-en-1-yl]carbamate 
• 89985-86-4 (R)-2-(N-tert-butoxycarbonylamino)-3-buten-1-ol 
• 91028-39-6 L-2-<<(tert-Butyloxy)carbonyl>amino>-3-butenoic Acid 
• 852693-74-4 methyl (S)-2-(tert-bytoxycarbonylamino)but-3-enoate 
• 860264-43-3 6,10-anhydro-7,8,9,11-tetra-O-benzyl-6-N-benzyloxycarbonylamino-2-tert-butoxycarbonylamino-2,3,4,5,6-pentadeoxy-1-O,2-N-isopropylidene-L-erythro-L-galacto-undecitol 
• 860264-44-4 6,10-anhydro-7,8,9,11-tetra-O-benzyl-6-N-benzyloxycarbonylamino-2-tert-butoxycarbonylamino-2,3,4,5,6-pentadeoxy-1-O,2-N-isopropylidene-L-threo-L-galacto-undecitol 

Relevant academic research and scientific papers

A simplified route to the (R)-Garner aldehyde and (S)-vinyl glycinol

An improved procedure for the conversion of D-serine into tert-butyl (R)-4-formyl-2,2-dimethyloxazolidine-3-carboxylate [the (R)-Garner aldehyde] is described which can be carried out in four operationally simple steps in 88% overall yield. Elaboration of this aldehyde to vinyl glycinol is also described.

Short and efficient synthesis of a vinyl-substituted tricyclic erythromycin derivative

(Chemical Equation Presented) Tricyclic erythromycin A derivatives are known potent antibacterial agents, but the potential of substituted tricyclic erythromycin A derivatives remains largely unexplored. To study this lead, the tricyclic ring system was synthesized by an efficient three-step synthesis starting from the allylic alcohol utilizing a novel azidoisocyanate. These tricyclic analogues can be used as scaffolds to probe secondary ribosomal binding sites.

Efficient conversion of (S)-methionine into (R)-garner aldehyde

An efficient method has been developed for the conversion of L-methionine into N,O-protected D-serinal (Garner aldehyde) in good overall yield.

PRODRUGS OF GLUTAMINE ANALOGS

Prodrugs of glutamine analogs, such as prodrugs of acivicin, are disclosed.

MACROCYCLIC LRRK2 KINASE INHIBITORS

The present invention relates to novel macrocyclic compounds of formula (I) and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.

SURVIVAL BENEFIT IN PATIENTS WITH SOLID TUMORS WITH ELEVATED C-REACTIVE PROTEIN LEVELS

This application relates to methods of increasing survival or progression-free survival in a patient with a solid tumor, wherein the patient has an elevated serum concentration of C-reactive protein (CRP), by administering a JAK inhibitor or an inhibitor of IL-6 signaling to the patient, as well as methods of predicting survival benefit in these patients from such therapy.

TREATMENT OF B-CELL MALIGNANCIES BY A COMBINATION JAK AND PI3K INHIBITOR

This invention relates to methods of treating B-cell malignancies using a combination of inhibitors of JAK1 and/or JAK2 and inhibitors of PI3Kδ.

BICYCLIC HETEROARYLAMINOALKYL PHENYL DERIVATIVES AS PI3K INHIBITORS

This application relates to derivatives of Formula I: and pharmaceutically acceptable salts thereof, which are inhibitors of PI3K, and compositions and methods of treatment related thereto.

TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1

This invention relates to JAK selective inhibitors for use in treatment of chronic neutrophilic leukemia and atypical chronic myeloid leukemia in patients.

MACROCYCLES AS PIM INHIBITORS

The invention relates to compounds of formula (1), 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.