35 results about "Nitrogen mustard derivative" patented technology

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

The invention relates to pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or medical salts thereof, as well as application of the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives or the medical salts thereof. The pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have the structure shown as the formula I. Pharmacological experiments show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives and the medical salts thereof have inhibiting effects on the proliferation of various tumor cells. Moreover, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are small in toxicity, have the advantages of selectivity on tumor cells, and are dual-functional anti-tumor drugs. Meanwhile, the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives are easy to synthesize, and the overall yields are high. All the advantages show that the pyrazolo[1,5-alpha] pyrimidine nitrogen mustard derivatives have great potential of being anti-tumor drugs.

The invention specifically discloses the structural formula of an arylamine nitrogen mustard derivative N,N-bis(2-chloroethyl)-N'-acetyl-1,4-phenylenediamine; and a preparation method thereof: firstly prepare N,N -bis(2-chloroethyl)-1,4-phenylenediamine; then charged with N,N-bis(2-chloroethyl)-1,4-phenylenediamine, dichloromethane and triethylamine In the reactor, the ice-water bath was cooled, stirred, and the mixed solution of acetyl chloride and dichloromethane was added dropwise to the reactor. After the dropwise addition was completed, the ice-water bath was removed, and the reaction was performed at room temperature for 2-14 hours. After the reaction was complete, washing, Dry, distill, and purify the filtered cake after distillation. On the premise of enhancing the therapeutic index of nitrogen mustard, the arylamine nitrogen mustard derivative of the present invention can effectively reduce the toxic and side effects of nitrogen mustard, and at the same time has the curative effect of bactericidal and anti-inflammatory, so as to reduce the reduction of immunity caused by patients after chemotherapy. risk of complications.

The invention belongs to the field of natural medicine and medicinal chemistry and relates to a scutellarin aglycone nitrogen mustard derivative and a preparation method and application thereof, in particular to a scutellarin aglycone nitrogen mustard derivative of which 4'-OH is combined with benzoic acid nitrogen mustard and a preparation method and antitumor activity thereof. The structure of the scutellarin aglycone nitrogen mustard derivative and pharmaceutically acceptable salt thereof is as shown in the general formula I, wherein R and n are as described in claims and the specification.The formula I is shown in the description.

The present invention provides a process for the production of compound (III) or a deprotected product thereof: comprising reacting compound (II) with chloroacetic acid, in the presence of a reducing agent; wherein PG is a protecting group and R is OH in a suitably protected form or (A). The invention further provides intermediate compounds formed in the process of the invention, and processes for the production of intermediate compounds.

The invention specifically discloses the structural formula of an arylamine nitrogen mustard derivative N,N-bis(2-chloroethyl)-N'-benzoyl-1,4-phenylenediamine; and a preparation method thereof: firstly, N, N-bis(2-chloroethyl)-1,4-phenylenediamine; N,N-bis(2-chloroethyl)-1,4-phenylenediamine, dichloromethane and triethylamine were then charged into the reactor, cooled in an ice-water bath, stirred, and added dropwise the mixed solution of benzoyl chloride and dichloromethane to the reactor, after the dropwise addition was completed, removed the ice-water bath, and reacted at room temperature for 8-14 hours, after the reaction was complete , the reaction solution is washed, dried, and distilled at atmospheric pressure successively, and the filter cake after distillation is purified, that is, it is obtained. Under the premise of enhancing the therapeutic index of nitrogen mustard, the arylamine nitrogen mustard derivative of the present invention can effectively reduce the toxic and side effects of nitrogen mustard, and has the curative effect of bactericidal and anti-inflammatory at the same time, so as to reduce the reduction of immunity caused by patients after chemotherapy. risk of complications.

The invention specifically discloses the structural formula of a nitrogen mustard derivative N,N-di(2-chloroethyl)-N'-tetradecanoyl-1,4-phenylenediamine; and a preparation method thereof: firstly prepare N, N-bis(2-chloroethyl)-1,4-phenylenediamine; then N,N-bis(2-chloroethyl)-1,4-phenylenediamine, dichloromethane and triethylamine into the reactor, cooled in an ice-water bath, stirred, and added dropwise a mixed solution of myristyl chloride and dichloromethane to the reactor, after the dropwise addition was completed, the ice-water bath was removed, and the room temperature was reacted for 10-14 hours. After the reaction was complete, The reaction solution is washed, dried with anhydrous copper sulfate, and distilled at normal pressure, and the distilled filter cake is purified to obtain the obtained product. Under the premise of enhancing the nitrogen mustard therapeutic index, the nitrogen mustard derivatives of the present invention can effectively reduce the toxic and side effects of the nitrogen mustard, and at the same time have the curative effects of sterilization and anti-inflammation, so as to reduce the symptoms caused by the decreased immunity of patients after chemotherapy. risk of complications.

The invention relates to the fields of natural medicine and medicinal chemistry, and relates to a preparation method and application of a 4-position spliced ​​melphalan nitrogen mustard derivative of brefeldin A. It specifically relates to the preparation method of introducing DNA alkylating agent melphalan derivatives into the 4-OH site of brefeldin A and its application in the preparation of antitumor drugs. The structure of the 4-position melphalan nitrogen mustard derivative of brefeldin A according to the present invention and its pharmaceutically acceptable salt is shown in the general formula I, wherein, n is as in the claims and description mentioned.

The novel nitrogen mustard derivative is characterized in that: one end has a nitrogen mustard alkylating group; the other end has a 6,7-substituted quinazoline structure, and the substituent R1 is located at the 4-position of the quinazoline parent, which is 2- or 3 - the nitrogen mustard group; the 6 and 7 positions of the quinazoline parent are morpholine propoxy and methoxy. The structure is as formula A. Experiments show that this kind of compound can inhibit cell cycle in G2 / M phase, and is a kind of bifunctional alkylating agent. Anti-tumor activity experiments in vivo show that the compound has good activity. Not only that, this type of compound also has the advantage that nitrogen mustards do not have, namely less toxicity. Simultaneously, the compounds are easy to synthesize, and the total yield is high. Various advantages show that this kind of compound has great potential to be a tumor treatment drug.

The invention relates to the fields of natural medicine and medicinal chemistry, in particular to a preparation method and application of a 7-position spliced ​​nitrogen mustard derivative of brefeldin A with antitumor activity. The structure of the nitrogen mustard derivative at the 7-position of brefeldin A according to the present invention and its pharmaceutically acceptable salt is shown in the following general formula I, wherein, n is as described in the claims and description.