862372-14-3

Upstream product

• 3262-72-4 (R)-N-tert-butoxycarbonyl serine 
• 74-88-4 methyl iodide 
• 86123-95-7 (R)-2-((tert-butoxycarbonyl)amino)-3-methoxypropionic acid 
• 420-37-1 trimethoxonium tetrafluoroborate 
• 95715-85-8 2-(tert-butoxycarbonylamino)-3-hydroxypropionic acid methyl ester 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1800300-79-1 methyl (2R)-2-amino-3-methoxypropanoate hydrochloride 
• 4530-20-5 BOC-glycine 

Downstream Products

• 721927-59-9 tert-butyl [(2R)-1-hydroxy-3-methoxypropan-2-yl]carbamate 
• 86123-95-7 (R)-2-((tert-butoxycarbonyl)amino)-3-methoxypropionic acid 

Relevant academic research and scientific papers

Cycloalkyl and heterocycloalkyl inhibitors as well as preparation method and application thereof

The invention relates to cycloalkyl and heterocycloalkyl inhibitors as well as a preparation method and application thereof. Specifically, the compounds disclosed by the invention have a structure as shown in a formula (I). The invention also discloses a preparation method of the compounds and application of the compounds as KRASG12C inhibitors. The compounds have a good selective inhibition effect on KRASG12C, and have better pharmacodynamic and pharmacokinetic properties and lower toxic and side effects.

Preparation method of lacosamide

The invention provides a novel methylation method of a lacosamide synthesis intermediate, which comprises the following steps: methylating a compound I in a reaction solvent at a proper temperature byusing trimethyloxyonium tetrafluoroborate as a methylation reagent under alkaline condition to obtain a methylation product II. The reaction formula is shown in the specification. The method has theadvantages of mild reaction condition, simple post-treatment, green methylation reagent, no high toxicity and high reaction yield, and conforms to the safe and environment-friendly green chemical concept. The method is suitable for laboratory small-scale preparation and large-scale industrial production.

Biosurfactants from Marine Cyanobacteria Collected in Sabah, Malaysia

Chemical investigation of the organic extract from Moorea bouillonii, collected in Sabah, Malaysia, led to the isolation of three new chlorinated fatty acid amides, columbamides F (1), G (2), and H (3). The planar structures of 1-3 were established by a combination of mass spectrometric and NMR spectroscopic analyses. The absolute configuration of 1 was determined by Marfey's analysis of its hydrolysate and chiral-phase HPLC analysis after conversion and esterification with Ohrui's acid, (1S,2S)-2-(anthracene-2,3-dicarboximido)cyclohexanecarboxylic acid. Compound 1 showed biosurfactant activity by an oil displacement assay. Related known fatty acid amides columbamide D and serinolamide C exhibited biosurfactant activity with critical micelle concentrations of about 0.34 and 0.78 mM, respectively.

Preparation method of R-2-acylamino-3-methyl methoxypropionate

The invention discloses a preparation method of R-2-acylamino-3-methyl methoxypropionate shown in a formula (I). The preparation method is characterized by comprising the following steps: firstly, enabling N-acyl protected glycine, which is used as a raw material and shown in a formula (II), bis(trichloromethyl) carbonate (III) and N, N-disubstituted formamide shown (IV) to be subjected to a cyclization reaction so as to obtain an intermediate (V); then, carrying out alkali treatment, acid ring-opening and methyl etherification to obtain an intermediate (VII); finally, carrying out asymmetrichydrogenation reduction to generate a target product (I). The preparation method provided by the invention has the advantages that the raw materials are simple and easy to obtain, the cost is low, reaction conditions are mild, the yield is high, the aftertreatment is simple, three wastes are less, and the economic benefit is good, thus being an environment-friendly process suitable for industrialproduction. (The formulas (I), (II), (III), (IV), (V), (VI) and (VII) are shown in the description.).

FUSED MORPHOLINOPYRIMIDINES AND METHODS OF USE THEREOF

The present disclosure relates to Fused Morpholinopyrimidines, pharmaceutical compositions comprising an effective amount of a Fused Morpholinopyrimidine and methods for using a Fused Morpholinopyrimidine in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of a Fused Morpholinopyrimidine.

Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria

An innovative approach was developed for the discovery of new natural products by combining mass spectrometric metabolic profiling with genomic analysis and resulted in the discovery of the columbamides, a new class of di- and trichlorinated acyl amides with cannabinomimetic activity. Three species of cultured marine cyanobacteria, Moorea producens 3L, Moorea producens JHB, and Moorea bouillonii PNG, were subjected to genome sequencing and analysis for their recognizable biosynthetic pathways, and this information was then compared with their respective metabolomes as detected by MS profiling. By genome analysis, a presumed regulatory domain was identified upstream of several previously described biosynthetic gene clusters in two of these cyanobacteria, M. producens 3L and M. producens JHB. A similar regulatory domain was identified in the M. bouillonii PNG genome, and a corresponding downstream biosynthetic gene cluster was located and carefully analyzed. Subsequently, MS-based molecular networking identified a series of candidate products, and these were isolated and their structures rigorously established. On the basis of their distinctive acyl amide structure, the most prevalent metabolite was evaluated for cannabinomimetic properties and found to be moderate affinity ligands for CB1. (Chemical Equation Presented)

QUINAZOLINE DERIVATIVES

A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.