5265-18-9

The invention relates to the field of cathinone artificial antigen structures, and particularly relates to a cathinone artificial antigen, an artificial antigen as well as a preparation method and application thereof. The cathinone artificial antigen is characterized in that a molecular structural formula of the cathinone artificial antigen is shown as follows: the formula (1) is shown in the description. According to the cathinone artificial antigen provided by the invention, a connecting arm is introduced onto a site N of cathinone, and the connecting arm is introduced onto the decoration site so that a characteristic structure of the cathinone is kept to a maximum extent; moreover, the cathinone artificial antigen has an active group coupled with carrier protein and can be used as an antigen determinant group. Compared with an annular connecting arm, the connecting arm adopted by the invention is chain-shaped, an identification degree of T cells to the connecting arm can be reducedas much as possible during immunization, so that an antibody obtained by immunization has higher specificity and affinity to the cathinone.

We report an enzymatic route for the formal regio- and stereoselective aminohydroxylation of β-methylstyrene that consumes only dioxygen, ammonia and formate; carbonate is the by-product. The biocascade entails highly selective epoxidation, hydrolysis and hydrogen-borrowing alcohol amination. Thus, β-methylstyrene was converted into 1R,2R and 1S,2R-phenylpropanolamine in 59-63% isolated yields, and up to >99.5 : 0.5 dr and er.

An expedient one-pot synthesis of aromatic amides has been reported from styrenes in the presence of N-bromosuccinimide and iodine by using aqueous ammonia in water. The reaction proceeds through the formation of α-bromoketone as an intermediate in the pr

The functionalization of carbonyl compounds in the α-position has gathered much attention as a synthetic route because of the wide biological importance of such products. Through polarity reversal, or "umpolung", we show here that typical nucleophiles, such as oxygen, nitrogen, and even carbon nucleophiles, can be used for addition reactions after tethering them to enol ethers. Our findings allow novel retrosynthetic planning and rapid assembly of structures previously accessible only by multistep sequences. A Nu approach: An efficient α-functionalization of ketones with a range of simple and useful nucleophiles is possible by using hypervalent iodine reagents (see scheme; Nu′ can be the Nu itself or a protected form of this nucleophile group).

The ultracentennial 10-I-4 iodinane oxide IBX (3; o-iodoxybenzoic acid; 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide) represents a new oxidizing reagent that successfully joins to the large family of known oxidants.IBX, in contrast to other valuable oxidants, is inexpensive to prepare and easy to handle, can tolerate moisture and water, and generally gives very good yields.Furthermore, IBX is mild and chemoselective (primary alcohols are converted into aldehydes with no overoxidation to acids; 1,2-diols are converted to α-ketols or α-diketones without oxidative cleavage; amino alcohols are oxidized to amino carbonyls, without protection of the amino group; sensitive heterocycles are not affected; various other functional groups are compatible with IBX oxidation).IBX is versatile (it works in various solvents and it is highly sensitive to temperature variations), and its solutions in DMSO are stable enough to carry out the oxidation reaction easily.