The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

The present invention discloses a hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d: ##STR00001## The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M.sup.−1cm.sup.−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

A dibromobenzyl derivative with a structure shown as formula I, a stereoisomer or a pharmaceutically acceptable salt thereof and a preparation method and an application of the dibromobenzyl derivative are provided. The dibromobenzyl derivative or the stereoisomer thereof is superior in in-vivo pharmacokinetic stability and drug efficacy, and capable of being used for preparing respiratory drugs, in particular the apophlegmatic drugs.

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A dibromobenzyl derivative with a structure shown as formula I, a stereoisomer or a pharmaceutically acceptable salt thereof and a preparation method and an application of the dibromobenzyl derivative are provided. The dibromobenzyl derivative or the stereoisomer thereof is superior in in-vivo pharmacokinetic stability and drug efficacy, and capable of being used for preparing respiratory drugs, in particular the apophlegmatic drugs.

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Provided herein are methods of preparation of I by reacting i with acid where R.sub.1 and R.sub.2 are each independently a leaving group. Intermediates to make i are also claimed. ##STR00001##

Provided herein are methods of preparation of I by reacting i with acid where R.sub.1 and R.sub.2 are each independently a leaving group. Intermediates to make i are also claimed. ##STR00001##

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent.

##STR00001##

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent.

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