Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.

The present invention provides a process for preparing 2-methyl-N-(2′-methylbutyl)butanamide of the following formula (1):the process comprising: subjecting an α-arylethyl-2-methylbutylamine compound of the following general formula (2): wherein Ar represents a substituted or unsubstituted aryl group having 6 to 20 carbon atoms, to N-2-methylbutyrylation to form an N-α-arylethyl-2-methyl-N-(2′-methylbutyl)butanamide compound of the following general formula (3): wherein Ar is as defined above, and removing the α-arylethyl group of the resulting compound (3) to form 2-methyl-N-(2′-methylbutyl)butanamide (1).

##STR00001##

The invention relates to the field of pharmaceutical synthesis, in particular to a preparation method of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives and their intermediates. The preparation method is carried out starting from compound Formula A1. ##STR00001## In the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol derivatives, the chirality was constructed by enzymatic method, and the products were prepared with high optical purity. The preparation method can be used to produce the key intermediates of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol of darunavir commercially, which is a very economical route suitable for industrial production.

A preparation method of an intermediate compound of formula II ((1R,2S,3S,4S,5S,6R,11S,14S,17S,19R,21R,23S,25R,26R,27S,31R,34S)-25-[(2S)-2,3-dihydroxy]-2,5-di hydroxy-26-methoxy-19-methyl-13,20-dimethylene-24,35,36,37,38,39-hexaoxane[29.3.1.1.sup.3,6.1.sup.4,34.11.sup.1,14.1.sup.17,21.0.sup.23,27]nonatriacontan-8,29-dione) for eribulin mesylate is provided, including subjecting a compound of formula I to a reaction with an additive in the presence of tetra-n-butylammonium fluoride (TBAF). The additive is piperidine hydrochloride or pyridine hydrochloride, and a reaction formula is as follows:

##STR00001##

The present invention aims to avoid the problem that a traditional synthetic route has a low yield.

The present application discloses a 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based phosphine ligand, an intermediate, a preparation method and uses thereof. The compound of phosphine ligand is a compound having a structure represented by formula I or formula II, or an enantiomer, a raceme, or diastereomer thereof. The phosphine ligand can be prepared via a preparation scheme in which the cheap and easily available 6,6′-dihydroxyl-3,3,3′,3′-tetramethyl-1,1′-spirobiindane is used as a raw material and the compound represented by formula III serves as the key intermediate. The new phosphine ligand developed by the present application can be used in catalytic organic reaction, in particular as a chiral phosphine ligand that is widely used in many asymmetric catalytic reactions including asymmetric hydrogenation and asymmetric allyl alkylation, and thus it has economic practicability and industrial application prospect. ##STR00001##

Provided herein are methods and compounds for targeted autophagy.

A nitrogen-containing derivative of substituted phenol hydroxyl acid ester is represented by formula (I). A salt of the compound of formula (I) has good water solubility, and in vivo, can rapidly and completely release substituted phenols having a pharmacological effect, which can improve the water solubility of substituted phenols, rapidly exert the pharmacological effects of substituted phenols in vivo, and has good safety. The method for preparing the above-mentioned compound is provided. This compound can also be used in the preparation of drugs that produce anaesthesia and/or sedative and hypnotic effects on humans and animals.

##STR00001##

The present invention relates to a process for resolution of Chlocyphos of Formula (I) to obtain corresponding (S)- or (R)-isomers. The present invention further relates to a process of obtaining (S)-Chlocyphos using (R)-(+)-α-methylbenzylamine and (R)-Chlocyphos using (S)-α-methylbenzylamine. The said resolution process provides the corresponding isomer with chiral purity more than 98%.

##STR00001##

Described herein are compounds of the formulae (I)-(III) as well as pharmaceutical compositions comprising such compounds and methods for using such compounds/pharmaceutical compositions for treating Alzheimer's disease.

The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam. ##STR00001##