Court states that it would not have been obvious to those of ordinary skill in the art to choose the particular acid claimed as an acylating
agent for the known amine simply because the particular acid was unknown except for Ochiai's disclosure in the patent application.
This new technology may have to await additional work, as the safety and toxicology of chemically reactive agents themselves (several alkylating agents, diazonium compounds and acylating
agents are known to have carcinogenic, mutagenic, skin sensitizing and allergenic properties), and the FDA status of chemically modified drug active ingredients (such as sunscreen active ingredients) after such ingredients have been attached to human skin.
Recently, we (Zou et al., 1997) have confirmed that the yeast (Saccharomyces cerevisiae) SLC1-1 gene encodes an sn-2 acyltransferase capable of acylating
sn-1-oleoyl-lysophosphatidic acid using a range of acyl-CoA thioesters, including 22:1-COA.
To compensate for possible differences in the reactivity of the acylating
agent with primary and secondary amines, differing detector responses toward the amide derivatives formed with each analyte, and the expected differences in biofluid concentrations of MDMA and MDA, we deemed it appropriate to select two internal standards.
Reactions of aromatic N-oxides with enamines of cyclohexanone in the presence of acylating
In a study of various lignins derived from brewer's spent grain, 2D HSQC NMR revealed the substructures including [beta]-O-4 alkyl-aryl ethers (77-79%), [beta]-5 phenylcoumarans (11-13%), [beta]-[beta]' resinols (5-6%), and 5-5' dibenzodioxocins (3-5%); while 2D HMBC NMR and derivatization followed by reductive cleavage analyses showed that p-coumarates were acylating
at the y-position of lignin side chains and were mostly occurred in condensed structures .
However, a careful examination of the data  shows that the discrimination against the modification of the a-amino group occurred only with bulky acylating
When comparing the results obtained in EPG85-257 cells for compounds 1-4, it can be suggested that the presence of acylating
groups at C-3 and C-16 is important for the cytotoxic activity of lathyrane diterpenes in multidrug-resistant EPG85-257RDB cells, since the presence of free hydroxyl groups at these positions decreased the activity.
The compound 1 (30 mg) was subjected to kinetic resolution in dry hexane (6 mL) using 6 different lipases (5 or 1 mg), and the vinyl acetate (1.1 eq.) as the acylating
agent, at 30[degrees]C under continuous stirring (150 rpm) in an orbital shaker.
Ester interchange involving alkyl esters have been described rather slow and required a large excess of acylating
agent to shift the equilibrium towards formation of the desired compound .
It was found that three acylating
agents (acetic anhydride and s uccinic anhydride and benzoyl chloride) and ( -)-a rctigenin were added into the methylene dichloride heated at 38-40 and acylations were performed at the C -OH (C4') (Sche me-2).
Pasini, "The acylating
potential of gamma-lactam antibacterials: base hydrolysis of bicyclic pyrazolidinones," Journal of Medicinal Chemistry, vol.