149182-70-7

Upstream product

• 100-59-4 phenylmagnesium chloride 
• 178432-72-9 (S)-2-tert-Butylcarbamoyl-aziridine-1-carboxylic acid tert-butyl ester 
• 2130-96-3 O-benzyl-N-tert-butoxycarbonyl-L-tyrosine 
• 94790-37-1 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 63-91-2 L-phenylalanine 
• 3262-72-4 (S)-N-(tert-butoxycarbonyl)serine 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 10017-37-5 tert-butylamine hydrochloride 
• 75-64-9 tert-butylamine 
• 3674-06-4 Boc-Phe-ONSu 

Downstream Products

• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 908253-03-2 (S)-N-tert-butyl-3-phenylpropane-1,2-diamine 
• 17186-52-6 H-Phe-NH-tert-butyl hydrochloride 
• 142580-70-9 [(1S,2R)-1-Benzyl-3-((S)-1-tert-butylcarbamoyl-2-phenyl-ethylamino)-2-hydroxy-propyl]-carbamic acid tert-butyl ester 
• 714970-51-1 [2-[2-(1-tert-butylcarbamoyl-2-phenyl-ethylcarbamoyl)-pyrrolidin-1-yl]-1-(4-hydroxy-benzyl)-2-oxo-ethyl]-carbamic acid tert-butyl ester 
• 714970-23-7 2-(1-tert-butylcarbamoyl-2-phenyl-ethylcarbamoyl)-pyrrolidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Homoserine and Threonine Peptide Assembly

Drawing on our recent success with reagent-less peptide-bond formation through serine-based assembly reactions in organic solvent, their range has been expanded to threonine and homoserine (an aspartic acid precursor) in the N -terminal peptide. Amino aci

Hydrogen Bonded Squaramide-Based Foldable Module Induces Both β- And α-Turns in Hairpin Structures of α-Peptides in Water

A novel tertiary squaramido-based reverse-turn module SQ is reported, and its conformational properties are evaluated. This module is easily incorporated into a α-peptide sequence by conventional solid-phase peptide synthesis. The structure characterizati

Supramolecular Interlocked Biphenyl Ligands for Enantioselective Ti-Catalyzed Alkylation of Aromatic Aldehydes

The substitution of tropos 2,2′-biphenols with (S)-amino-acid-derived interaction sites in the 5,5′-position results in a spontaneous desymmetrization. This process is driven by well-defined intermolecular hydrogen bonding, which leads to diastereoselecti

Inducing Enantioselectivity in a Dynamic Catalyst by Supramolecular Interlocking

The design of a new class of fluxional biphenyl bisphosphinite (BIBIPHOS) ligands decorated with amino acid-based diamide interaction sites is reported that undergo spontaneous desymmetrization. Hydrogenation of prochiral alkenes using Rh-BIBIPHOS results

DERIVATIVES OF DOLASTATIN 10 AND USES THEREOF

Derivatives of dolastatin 10 and uses thereof, the structures of which are shown as formula I, II, III and IV are provided.

Highly enantioselective epoxidation of α,β-unsaturated ketones catalyzed by primary-secondary diamines

The asymmetric epoxidation of α,β-unsaturated ketones has been achieved by using functional and readily accessible primary-secondary diamines as the catalysts, giving the useful alkyl epoxy products with good yields and high enantioselectivities (up to 99% ee). Copyright

Efficient preparation of chiral diamines via Red-Al reduction of N-Boc-protected amino acid-derived secondary amides

Conditions have been developed for the selective reduction of N-Boc-protected amino acid-derived secondary amides, avoiding the formation of overreduction and cyclic urea byproducts. The method is showcased by the efficient formal synthesis of NK-1 antagonist LY303870.

Development of potent bifunctional endomorphin-2 analogues with mixed μ-/δ-opioid agonist and δ-opioid antagonist properties

The C terminus of endomorphin-2 (EM-2) analogues (Tyr-Pro-Phe-NH-X) was modified with aromatic, heteroaromatic, or aliphatic groups (X = phenethyl,benzyl, phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, tert-butyl, cyclohexyl, or adamantyl; 3-18) to study their effect on opioid activity. Only 9 (1-naphthyl), 11 (5-quinolyl), 16 (cyclohexyl), and 18 (2-adamantyl) exhibited μ-opioid receptor affinity in the nanomolar range (Ki = 2.41-6.59 nM), which, however, was 3-to 10-fold less than the parent peptide. Replacement of Tyr1 by Dmt (2′,6′-dimethyl-L-tyrosine) (19-32) exerted profound effects: (i) acquisition of high μ-opioid receptor affinity (Ki = 0.11-0.52 nM) except 23 (Ph); (ii) presence of potent functional μ-opioid receptor agonism (IC50 1]EM-2), 27 (1-naphthyl), 29 (5-quinolyl), and 32 (5-isolquinolyl); (iii) association of weak δ-opioid antagonist activity (pA2 = 5.41-7.18) except 19 ([Dmt1]EM-2), 20 (H), 27 (1-naphthyl), and in particular 29 (5-quinolyl) with its potent δ-agonism (IC50 = 0.62 nM, pA2 = 5.88); (iv) production of antinociception after ic administration of 32 (5-isoquinolyl) in mice, a bioactivity absent in the corresponding Tyr1 analogue (14); and (v) preferential cis orientation (cis/trans = 3:2 to 7:3) at the Dmt-Pro amide bond, in contrast to the Tyr-Pro amide trans orientation (cis/trans = 1:2 to 1:3). Thus, [Dmt1]EM-2 analogues with hydrophobic C-terminal extensions provide model compounds with potent μ-opioid receptor bioactivity and dual functional agonism.

Peptidyl calcium channel blockers

The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

TYROSINE-DERIVED COMPOUNDS AS CALCIUM CHANNEL ANTAGONISTS

The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, whereinR 1 and R 2 are independently H, phenylcyclopentylcarbonyl, C 1-C 7 alkyl, cyclohexyl