摘要:
A process for the preparation of &bgr;,γ-unsaturated-γ, γ-disubstituted esters 1 with high E/Z- and &bgr;,γ/α,&bgr;-ratios, Formula (1) by reacting at a temperature of between about 130 and 170 degrees centigrade the conjugated malonate Formula (3) with, a group I, II or III metal halide or an organic cation/halide anion pair, an inorganic proton source and a polar solvent.
摘要:
The invention relates to a method for producing 2-halogen-acrylic acid esters from 2-hydroxymethyl- or 2-halogen-methyl- or 2-chlorosulfinyloxymethyl-2-halogen-malonic acid diesters. The invention further relates to 2-halogen-methyl-2-halogen-malonic acid diesters or 2-chlorosulfinyloxymethyl-2-halogen-malonic acid diesters of a new type, which can be used to produce the 2-halogen-acrylic acid esters.
摘要:
Provided is a short process for simply and efficiently producing 3,5-dimethyldodecanoic acid, which is an active ingredient of the pheromone of California prionus. More specifically provided is a method for producing 3,5-dimethyldodecanoic acid (5) comprising the steps of: converting 2-methylnonyl halide (1) to a 2-methylnonyl metal reagent (2), and reacting the 2-methylnonyl metal reagent (2) with 2-ethylidene malonic acid ester (3) to form 2-(1,3-dimethyldecyl)malonic acid ester (4) as a result of 1,4-addition of the 2-methylnonyl metal reagent (2) to the 2-ethylidene malonic acid ester (3), as shown in the following scheme:
摘要:
A process for the preparation of β,γ-unsaturated-γ,γ-disubstituted esters 1 with high E/Z - and β,γ/α,β-ratios, Formula (1) by reacting at a temperature of between about 130 and 170 degrees centigrade the conjugated malonate Formula (3) with, a group I, II or III metal halide or an organic cation/halide anion pair, an inorganic proton source and a polar solvent.
摘要:
The present invention relates to intermediates useful in the synthesis of Dolasetron and synthetic precursors thereof, as well as to processes for obtaining them. In addition, it refers to the hydrochloric salt of Dolasetron and polymorphic forms of Dolasetron and precursors thereof.
摘要:
The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2'):
wherein R is a fluorine atom or a methoxy group, and R 400 is a hydrogen atom or a C 1 - C 4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
摘要:
To provide a process for producing a (4E)-5-chloro-2-isopropyl-4-pentenoate in high yield and efficiently. A compound (2) is reacted with a base in the presence of an aprotic solvent and then with (1E)-1,3-dichloro-1-propene in the same reaction vessel to obtain a compound (3), and then either of -COOR moieties in the compound (3) is replaced with a hydrogen atom in the same reaction vessel to obtain a compound (4):
wherein R is a lower alkyl group or an aralkyl group.
摘要:
Processes for producing a (4E)-5-chloro-2-isopropyl-4-pentenoic ester and an optically active isomer thereof which are useful as intermediates for medicines and agricultural chemicals. One of the processes, which is for producing a (4E)-5-chloro-2-isopropyl-4-pentenoic ester represented by the following formula (4), is characterized by reacting a compound represented by the following formula (2) with a base (II) in the presence of an aprotic solvent (II) and subsequently with (1E)-1,3-dichloro-1-propene to obtain a compound represented by the following formula (3) and then eliminating the alkoxycarbonyl group from one of the ester groups of the compound represented by the following formula (3). The other process, which is for producing an (S)-(4E)-5-chloro-2-isopropyl-4-pentenoic ester represented by the following formula (5), is characterized by optically resolving the (4E)-5-chloro-2-isopropyl-4-pentenoic ester represented by the formula (4), which is obtained by that production process. (In the formulae, R represents lower alkyl or aralkyl.)